Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
9815409 12258 17 None 1 2 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1185481 12258 17 None 1 2 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL416736 12258 17 None 1 2 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
1979 76973 66 None -2089 7 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 10.1021/jm960467d
CHEMBL20835 76973 66 None -2089 7 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 10.1021/jm960467d
2551 782 23 None 2 12 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 782 23 None -7 12 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
298 782 23 None -7 12 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
488 782 23 None -7 12 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
CHEMBL965 782 23 None -7 12 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
DB00411 782 23 None -7 12 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
9838581 11872 2 None 4 2 Mouse 6.0 pEC50 = 6.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1183042 11872 2 None 4 2 Mouse 6.0 pEC50 = 6.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL277014 11872 2 None 4 2 Mouse 6.0 pEC50 = 6.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
3652 4034 72 None -1737 9 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
57 4034 72 None -1737 9 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
60809 4034 72 None -1737 9 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
CHEMBL21536 4034 72 None -1737 9 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
DB15357 4034 72 None -1737 9 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
10703031 11046 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1178347 11046 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL22089 11046 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
44589681 184706 0 None -12 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL485913 184706 0 None -12 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
22745278 186480 1 None -53 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL491209 186480 1 None -53 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
306 3400 18 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3536 3400 18 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
53930639 3400 18 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
9577995 3400 18 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
CHEMBL134641 3400 18 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3652 4034 72 None -275 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 4034 72 None -275 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 4034 72 None -275 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 4034 72 None -275 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 4034 72 None -275 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
2551 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
1726 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
2230 461 55 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
296 461 55 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
CHEMBL7303 461 55 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
DB04365 461 55 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
10375030 13841 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL1196670 13841 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL557795 13841 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
2551 782 23 None 2 12 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
650899 54129 10 None -4 5 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1535797 54129 10 None -4 5 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1609153 54129 10 None -4 5 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
42599070 15902 0 None -316 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223804 15902 0 None -316 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598359 15930 0 None -100 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223864 15930 0 None -100 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
2551 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
9308 17572 16 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL1255785 17572 16 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL12587 17572 16 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL292911 17572 16 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
2551 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
156015300 177018 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177018 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
10012139 13598 10 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL1194965 13598 10 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL553602 13598 10 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
10240891 204378 0 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 140 1 0 3 0.3 CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL85678 204378 0 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 140 1 0 3 0.3 CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
2551 782 23 None 2 12 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 782 23 None -7 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
298 782 23 None -7 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
488 782 23 None -7 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
CHEMBL965 782 23 None -7 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
DB00411 782 23 None -7 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
42598360 15928 0 None -630 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223862 15928 0 None -630 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
9990434 105858 0 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL313918 105858 0 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
156021744 177540 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4648071 177540 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
92209180 13042 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
9793884 13042 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1190710 13042 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL541398 13042 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
124300908 13083 5 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
2606 13083 5 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1191029 13083 5 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL542065 13083 5 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
2551 782 23 None -7 12 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
298 782 23 None -7 12 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
488 782 23 None -7 12 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
CHEMBL965 782 23 None -7 12 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
DB00411 782 23 None -7 12 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
156015097 176978 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4640324 176978 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
2551 782 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 782 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
42598829 15904 0 None -251 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223806 15904 0 None -251 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598828 15927 0 None -1584 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223861 15927 0 None -1584 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
187 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
294 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
65 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
8593 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
CHEMBL667 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
DB03128 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
2551 782 23 None 2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
71737672 2539 14 None -3 6 Human 5.7 pEC50 = 5.7 Functional
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2539 14 None -3 6 Human 5.7 pEC50 = 5.7 Functional
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2539 14 None -3 6 Human 5.7 pEC50 = 5.7 Functional
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
44158142 188085 40 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
CHEMBL503735 188085 40 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
44158142 188085 40 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
CHEMBL503735 188085 40 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
2551 782 23 None -7 12 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
298 782 23 None -7 12 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
488 782 23 None -7 12 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
CHEMBL965 782 23 None -7 12 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
DB00411 782 23 None -7 12 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
16071018 15878 15 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223753 15878 15 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
42598357 15929 0 None -794 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223863 15929 0 None -794 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
16071018 15878 15 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL1223753 15878 15 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
3652 4034 72 None -275 9 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4034 72 None -275 9 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4034 72 None -275 9 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4034 72 None -275 9 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4034 72 None -275 9 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
71792 77998 32 None -6 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
CHEMBL2111051 77998 32 None -6 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
44251554 6983 0 None -1 4 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
CHEMBL1084941 6983 0 None -1 4 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
44422692 11748 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182296 11748 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL228144 11748 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
14235519 16379 8 None 4 2 Mouse 5.6 pEC50 = 5.6 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1 10.1021/jm960467d
CHEMBL12378 16379 8 None 4 2 Mouse 5.6 pEC50 = 5.6 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1 10.1021/jm960467d
187 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
294 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
65 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
8593 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
CHEMBL667 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
DB03128 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
187 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
8593 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
9815331 201417 1 None 3 5 Rat 8.4 pEC50 = 8.4 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 201417 1 None 3 5 Rat 8.4 pEC50 = 8.4 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
9883040 100071 0 None -3 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL291339 100071 0 None -3 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL542622 100071 0 None -3 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
2551 782 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 782 23 None 2 12 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
71737672 2539 14 None -5 6 Rat 5.5 pEC50 = 5.5 Functional
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2539 14 None -5 6 Rat 5.5 pEC50 = 5.5 Functional
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2539 14 None -5 6 Rat 5.5 pEC50 = 5.5 Functional
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
42599068 15903 0 None -100 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223805 15903 0 None -100 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42599071 15948 0 None -1258 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223939 15948 0 None -1258 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
319 1297 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1297 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1297 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1297 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1297 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1297 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
2551 782 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
42598586 15947 0 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223938 15947 0 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25207745 15950 0 None -398 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223941 15950 0 None -398 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44253016 80047 2 None -316 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
CHEMBL2146597 80047 2 None -316 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
16123945 80049 8 None -794 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
CHEMBL2146599 80049 8 None -794 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
156011965 176718 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 176718 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
2551 782 23 None 2 12 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
24865895 95559 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL259662 95559 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL390842 95559 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
2551 782 23 None 2 12 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
319 1297 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1297 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1297 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1297 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1297 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1297 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
2551 782 23 None 2 12 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
298 782 23 None 2 12 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
488 782 23 None 2 12 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
CHEMBL965 782 23 None 2 12 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
DB00411 782 23 None 2 12 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
367 3764 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
5487427 3764 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
8592 3764 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL1900528 3764 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL3305968 3764 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL4650755 3764 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
DB01409 3764 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
10197743 12836 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
92209179 12836 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1189286 12836 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL538467 12836 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
2551 782 23 None -7 12 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 782 23 None -7 12 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 782 23 None -7 12 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 782 23 None -7 12 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 782 23 None -7 12 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
44422699 11746 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182272 11746 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL227378 11746 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
44422692 11748 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182296 11748 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL228144 11748 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
10727260 11883 0 None 2 2 Mouse 5.2 pEC50 = 5.2 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1183133 11883 0 None 2 2 Mouse 5.2 pEC50 = 5.2 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL281411 11883 0 None 2 2 Mouse 5.2 pEC50 = 5.2 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
334 234 21 None -144 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
9928284 234 21 None -144 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
CHEMBL2022960 234 21 None -144 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
644390 40171 6 None -2 4 Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
CHEMBL1482157 40171 6 None -2 4 Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
156014812 177687 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4647437 177687 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650736 177687 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156009673 177679 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4633816 177679 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650683 177679 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156015300 177018 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177018 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
42598591 15901 0 None -125 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223803 15901 0 None -125 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25230693 15949 0 None -251 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223940 15949 0 None -251 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
3008304 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
7632 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
CHEMBL523685 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
147230103 179573 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
CHEMBL4748915 179573 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
3008304 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
7632 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
CHEMBL523685 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
3008304 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
7632 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
CHEMBL523685 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
2551 782 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 782 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
135409468 2004 63 None -13 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
333 2004 63 None -13 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
CHEMBL845 2004 63 None -13 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
647412 27112 9 None -5 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
CHEMBL1367424 27112 9 None -5 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
24967746 15879 0 None -199 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223754 15879 0 None -199 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598358 15926 0 None -794 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223860 15926 0 None -794 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
10397133 106579 1 None -3 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 164 2 0 3 0.3 C#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL315676 106579 1 None -3 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 164 2 0 3 0.3 C#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
10397356 120204 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL354738 120204 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
10130070 119824 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 154 2 0 3 0.7 CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL352908 119824 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 154 2 0 3 0.7 CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
156011965 176718 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 176718 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
2551 782 23 None 2 12 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None 2 12 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None 2 12 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None 2 12 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None 2 12 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
10375322 58422 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 192 2 0 3 1.1 CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL168545 58422 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 192 2 0 3 1.1 CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
2551 782 23 None -93 12 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
298 782 23 None -93 12 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
488 782 23 None -93 12 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
CHEMBL965 782 23 None -93 12 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
DB00411 782 23 None -93 12 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
2551 782 23 None -7 12 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 782 23 None -7 12 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 782 23 None -7 12 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 782 23 None -7 12 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 782 23 None -7 12 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
5487543 203933 4 None -41 6 Human 5.4 pED50 = 5.4 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
CHEMBL81878 203933 4 None -41 6 Human 5.4 pED50 = 5.4 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
9795428 96041 4 None -20 5 Human 6.1 pED50 = 6.1 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
CHEMBL262455 96041 4 None -20 5 Human 6.1 pED50 = 6.1 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
11442478 105996 0 None 1 3 Human 9.0 pIC50 = 9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085073 105996 0 None 1 3 Human 9.0 pIC50 = 9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140113 105996 0 None 1 3 Human 9.0 pIC50 = 9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL5074216 212544 0 None - 1 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074599 212548 0 None - 1 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074216 212544 0 None - 1 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086393 213253 0 None - 1 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44589585 188305 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507375 188305 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555474 188305 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5074599 212548 0 None - 1 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44232700 106029 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084399 106029 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140218 106029 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
11341753 186720 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 8 2 4 4.1 CCOc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492978 186720 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 8 2 4 4.1 CCOc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11341940 186779 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 CC1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493328 186779 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 CC1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
11364721 192122 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 427 7 2 4 3.9 CC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522020 192122 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 427 7 2 4 3.9 CC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44589495 185398 0 None 10 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 5 7 3.8 CCCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL486982 185398 0 None 10 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 5 7 3.8 CCCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590173 188502 0 None -1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL510029 188502 0 None -1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555019 188502 0 None -1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076886 212696 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3C[C@H]4CC[C@H](C3)N4C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
71452454 83504 0 None 41 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 603 9 3 7 3.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206587 83504 0 None 41 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 603 9 3 7 3.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2012.09.085
11552174 103026 0 None 1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085090 103026 0 None 1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
11330061 186729 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492997 186729 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2009.01.098
44589570 172188 0 None 15 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 10 5 6 3.5 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL451040 172188 0 None 15 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 10 5 6 3.5 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589498 172189 0 None 3 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 572 11 5 7 3.8 O=C(Nc1ccc(C(=O)OCC2CC2)cc1)N[C@@H](Cc1ccc(O)cc1)C(=O)NC1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL451043 172189 0 None 3 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 572 11 5 7 3.8 O=C(Nc1ccc(C(=O)OCC2CC2)cc1)N[C@@H](Cc1ccc(O)cc1)C(=O)NC1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.09.020
44573500 187137 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1Cl 10.1016/j.bmcl.2009.01.098
CHEMBL495361 187137 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1Cl 10.1016/j.bmcl.2009.01.098
44589575 175070 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 596 9 4 7 2.9 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)N4CCOCC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL458105 175070 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 596 9 4 7 2.9 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)N4CCOCC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
145955917 161933 0 None -29 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 418 6 2 4 4.2 NC[C@H]1CC[C@H](CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
CHEMBL4167221 161933 0 None -29 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 418 6 2 4 4.2 NC[C@H]1CC[C@H](CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
44233187 85598 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2306159 85598 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233187 85598 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2306159 85598 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
76324336 103022 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085086 103022 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
76331543 103028 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 4 4.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085092 103028 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 4 4.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
57758637 106017 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084466 106017 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140183 106017 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44232702 106021 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3084401 106021 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3140203 106021 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
11547053 105984 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085074 105984 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140097 105984 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
145958296 161732 0 None -38 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4164075 161732 0 None -38 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
142416754 161792 0 None -112 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 480 8 2 4 5.2 FC1(F)CCC(NC/C=C\CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
CHEMBL4164874 161792 0 None -112 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 480 8 2 4 5.2 FC1(F)CCC(NC/C=C\CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
44232708 106004 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
CHEMBL3084407 106004 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
CHEMBL3140145 106004 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
76320693 103018 0 None 1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085082 103018 0 None 1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
76309756 103019 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 375 4 0 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085083 103019 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 375 4 0 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44590174 169490 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL444300 169490 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL466271 169490 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590177 188335 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507874 188335 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL554918 188335 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076535 212674 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
11699452 12512 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187080 12512 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL489626 12512 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
44590179 172148 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450538 172148 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553446 172148 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44573621 186629 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 477 8 2 4 5.5 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492391 186629 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 477 8 2 4 5.5 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2009.01.098
44573263 192548 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CN2CCNCC2)cc1-c1cccc(CNC(=O)c2ccc3c(c2)OCO3)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522992 192548 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CN2CCNCC2)cc1-c1cccc(CNC(=O)c2ccc3c(c2)OCO3)c1 10.1016/j.bmcl.2009.01.098
44590181 172992 0 None -25 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL453248 172992 0 None -25 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL551113 172992 0 None -25 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
162646559 179060 0 None -97 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@@H](C)C1 10.1021/acsmedchemlett.0c00626
CHEMBL4742997 179060 0 None -97 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@@H](C)C1 10.1021/acsmedchemlett.0c00626
71459724 83593 0 None 63 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2207177 83593 0 None 63 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
42626092 12526 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187132 12526 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL491246 12526 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
145956824 161711 0 None -1412 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.1 NCC1CC1CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4163770 161711 0 None -1412 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.1 NCC1CC1CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
44233417 85619 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2307674 85619 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233417 85619 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2307674 85619 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
76324303 102774 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.6 CN1[C@H]2CC[C@@H]1C[C@H](CCC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084394 102774 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.6 CN1[C@H]2CC[C@@H]1C[C@H](CCC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
76327870 102777 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 273 4 1 2 3.5 CCC(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1021/jm900736e
CHEMBL3084397 102777 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 273 4 1 2 3.5 CCC(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1021/jm900736e
76327903 103029 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 381 4 0 5 4.4 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085093 103029 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 381 4 0 5 4.4 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
76316969 106041 0 None -2 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085075 106041 0 None -2 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140262 106041 0 None -2 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
71455969 83516 0 None 3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 581 12 4 5 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206603 83516 0 None 3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 581 12 4 5 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
1765112 102773 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 307 3 1 2 3.8 CN1[C@H]2CC[C@@H]1C[C@H](C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084393 102773 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 307 3 1 2 3.8 CN1[C@H]2CC[C@@H]1C[C@H](C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
25034111 192815 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL526009 192815 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
16040727 168876 0 None -3 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL442672 168876 0 None -3 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL495102 168876 0 None -3 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590124 169227 0 None 39 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 4 6 4.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL443925 169227 0 None 39 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 4 6 4.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590172 169750 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL444688 169750 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL527216 169750 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590171 178171 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL468609 178171 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL554632 178171 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590125 183279 0 None 12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 530 10 4 6 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480878 183279 0 None 12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 530 10 4 6 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590170 187787 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL501348 187787 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553431 187787 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
25034111 192815 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL526009 192815 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
76309754 106039 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085062 106039 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3140260 106039 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
44589571 172018 0 None 10 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 580 11 5 6 3.5 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCC4CC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL448904 172018 0 None 10 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 580 11 5 6 3.5 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCC4CC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
71452456 83522 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 525 10 4 5 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(C)CCCCCC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206609 83522 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 525 10 4 5 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(C)CCCCCC2)cc1 10.1016/j.bmcl.2012.09.085
25034180 187828 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL502000 187828 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
44573744 187066 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 7 1 5 4.2 CCN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL494996 187066 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 7 1 5 4.2 CCN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44589573 188318 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 616 11 5 6 4.3 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507581 188318 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 616 11 5 6 4.3 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
11510358 106002 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085069 106002 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140143 106002 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44232947 105987 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
CHEMBL3084411 105987 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
CHEMBL3140100 105987 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
11664153 12648 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL1187845 12648 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL523767 12648 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
76324304 102775 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 322 4 1 3 3.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccn1)C2 10.1021/jm900736e
CHEMBL3084395 102775 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 322 4 1 3 3.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccn1)C2 10.1021/jm900736e
15945874 188179 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL505452 188179 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
44573578 186624 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 7 2 5 3.5 COC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492374 186624 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 7 2 5 3.5 COC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11455956 187018 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 463 7 2 5 3.1 CS(=O)(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494749 187018 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 463 7 2 5 3.1 CS(=O)(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44590033 183096 0 None 12 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480299 183096 0 None 12 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
15945874 188179 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL505452 188179 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589984 189964 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL518001 189964 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
1201549 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
333 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
7601 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL1201203 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL438151 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
DB00245 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL5076445 212670 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5078006 212757 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086393 213253 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44232953 102916 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
CHEMBL3084663 102916 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
44232953 102916 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
CHEMBL3084663 102916 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
71459689 83502 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 595 13 4 5 5.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206585 83502 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 595 13 4 5 5.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
44573264 186619 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2ccc(F)c(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL492359 186619 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2ccc(F)c(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573619 187019 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 7 3 4 3.6 CC(=O)Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494752 187019 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 7 3 4 3.6 CC(=O)Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11714747 187050 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 7 2 4 3.8 CN(C)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494950 187050 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 7 2 4 3.8 CN(C)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11578568 187051 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 6 3 4 3.3 Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494951 187051 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 6 3 4 3.3 Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44573661 187797 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 3 4 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(O)c1 10.1016/j.bmcl.2009.01.098
CHEMBL501486 187797 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 3 4 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(O)c1 10.1016/j.bmcl.2009.01.098
25034112 187809 0 None -1 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL501727 187809 0 None -1 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
11690968 106019 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085072 106019 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140185 106019 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
11518068 106024 0 None 1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085059 106024 0 None 1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140213 106024 0 None 1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
11583262 106015 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085060 106015 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140181 106015 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
69444105 103012 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085077 103012 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44233675 102903 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084639 102903 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233675 102903 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084639 102903 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
11712408 106040 0 None -1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3085067 106040 0 None -1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3140261 106040 0 None -1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
76327901 103020 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
CHEMBL3085084 103020 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
11508710 103025 0 None 1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085089 103025 0 None 1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
42626088 12515 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL1187091 12515 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL490236 12515 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
71450615 83517 0 None 1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 609 14 4 5 5.5 CC[N+](CC)(CCNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)Nc1ccc(C(=O)OC(C)C)cc1)Cc1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206604 83517 0 None 1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 609 14 4 5 5.5 CC[N+](CC)(CCNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)Nc1ccc(C(=O)OC(C)C)cc1)Cc1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.085
44232951 105988 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 378 4 1 1 5.3 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CCC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084416 105988 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 378 4 1 1 5.3 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CCC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140101 105988 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 378 4 1 1 5.3 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CCC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
10092649 192471 51 None -29 11 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 192471 51 None -29 11 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
145954567 161956 0 None -100 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 416 6 2 4 4.3 NCC1=C(CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CCCC1 10.1021/acsmedchemlett.7b00406
CHEMBL4167521 161956 0 None -100 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 416 6 2 4 4.3 NCC1=C(CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CCCC1 10.1021/acsmedchemlett.7b00406
76324335 103017 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085081 103017 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
10092649 192471 51 None -29 11 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 192471 51 None -29 11 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
71450617 83523 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 527 12 4 5 4.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206610 83523 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 527 12 4 5 4.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2012.09.085
44455159 97316 0 None -20 5 Rat 4.6 pIC50 = 4.6 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL271704 97316 0 None -20 5 Rat 4.6 pIC50 = 4.6 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
44234432 106003 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(Cl)c1)c1cccc(Cl)c1)C2 10.1021/jm900736e
CHEMBL3084402 106003 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(Cl)c1)c1cccc(Cl)c1)C2 10.1021/jm900736e
CHEMBL3140144 106003 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(Cl)c1)c1cccc(Cl)c1)C2 10.1021/jm900736e
44590180 172077 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 5.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL449640 172077 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 5.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540398 172077 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 5.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590167 178446 0 None 3 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 494 10 4 6 2.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL471214 178446 0 None 3 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 494 10 4 6 2.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590182 182569 0 None 12 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 532 9 5 7 3.0 COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL479526 182569 0 None 12 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 532 9 5 7 3.0 COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590034 189384 0 None 12 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(OC)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL517087 189384 0 None 12 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(OC)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
44573370 186865 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cc(-c2cccc(CN3CCNCC3)c2)ccc1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL493939 186865 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cc(-c2cccc(CN3CCNCC3)c2)ccc1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573662 186944 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 399 6 2 3 4.0 Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494410 186944 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 399 6 2 3 4.0 Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44573420 187026 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 465 7 2 6 3.0 O=S(=O)(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494778 187026 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 465 7 2 6 3.0 O=S(=O)(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44589497 174721 0 None 5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 11 5 7 4.0 CC(C)COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL457302 174721 0 None 5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 11 5 7 4.0 CC(C)COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
11285415 186618 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 458 6 1 4 3.9 C[N+]1(C)CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL492358 186618 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 458 6 1 4 3.9 C[N+]1(C)CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL538863 186618 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 458 6 1 4 3.9 C[N+]1(C)CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44573372 192687 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL524031 192687 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44589499 191245 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 540 9 5 6 2.7 CNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL519893 191245 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 540 9 5 6 2.7 CNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
11442669 73931 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023761 73931 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
76320694 103021 0 None 1 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3085085 103021 0 None 1 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
11617374 103013 0 None 2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085078 103013 0 None 2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
71455965 83506 0 None 3 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](Cc3ccc(Cl)cc3)(C(C)C)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206589 83506 0 None 3 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](Cc3ccc(Cl)cc3)(C(C)C)CC2)cc1 10.1016/j.bmcl.2012.09.085
44234194 102921 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084670 102921 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44234194 102921 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084670 102921 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
9044803 123586 9 None -1 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633650 123586 9 None -1 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
9044803 123586 9 None -1 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633650 123586 9 None -1 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
44233419 102924 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
CHEMBL3084674 102924 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
44233419 102924 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
CHEMBL3084674 102924 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
44232710 106012 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(F)c(F)c1)c1ccc(F)c(F)c1)C2 10.1021/jm900736e
CHEMBL3084408 106012 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(F)c(F)c1)c1ccc(F)c(F)c1)C2 10.1021/jm900736e
CHEMBL3140173 106012 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(F)c(F)c1)c1ccc(F)c(F)c1)C2 10.1021/jm900736e
11503336 106032 0 None -1 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085071 106032 0 None -1 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140242 106032 0 None -1 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL5078006 212757 0 None - 1 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
11557048 187070 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 497 8 2 5 3.4 CN1CCN(Cc2cccc(C(=O)NCc3cccc(-c4cccc(CN5CCNCC5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL495028 187070 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 497 8 2 5 3.4 CN1CCN(Cc2cccc(C(=O)NCc3cccc(-c4cccc(CN5CCNCC5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
11633399 12510 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 352 6 1 2 3.6 COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187077 12510 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 352 6 1 2 3.6 COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL489225 12510 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 352 6 1 2 3.6 COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
11318734 186747 0 None 5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 6 2 5 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL493079 186747 0 None 5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 6 2 5 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
11273131 192527 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)OCO3)cc1-c1cccc(CN2CCNCC2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522838 192527 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)OCO3)cc1-c1cccc(CN2CCNCC2)c1 10.1016/j.bmcl.2009.01.098
44590036 187793 0 None 6 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 10 4 8 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL501419 187793 0 None 6 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 10 4 8 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590176 188477 0 None -3 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 4.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL509614 188477 0 None -3 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 4.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555707 188477 0 None -3 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 4.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
24882532 94674 0 None -7 4 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255523 94674 0 None -7 4 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
44573265 186682 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(-c2cccc(CNC(=O)c3ccc4c(c3)OCO4)c2)cc1CN1CCNCC1 10.1016/j.bmcl.2009.01.098
CHEMBL492756 186682 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(-c2cccc(CNC(=O)c3ccc4c(c3)OCO4)c2)cc1CN1CCNCC1 10.1016/j.bmcl.2009.01.098
44573501 186730 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL492998 186730 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.01.098
44573663 186945 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 413 7 2 3 4.3 CCc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494411 186945 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 413 7 2 3 4.3 CCc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11421571 187034 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494836 187034 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573423 187069 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL495025 187069 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
44589529 185938 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 554 10 5 6 3.1 CCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL487764 185938 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 554 10 5 6 3.1 CCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
25034110 188180 0 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL505453 188180 0 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
11584660 92836 7 None -19 5 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic receptor M3Antagonist activity at human muscarinic receptor M3
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL244946 92836 7 None -19 5 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic receptor M3Antagonist activity at human muscarinic receptor M3
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
44573371 186904 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.7 Cc1ccc(-c2cccc(CN3CCNCC3)c2)cc1CNC(=O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494131 186904 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.7 Cc1ccc(-c2cccc(CN3CCNCC3)c2)cc1CNC(=O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
57758634 105982 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 421 6 0 1 6.5 C[N+]1(Cc2ccccc2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084465 105982 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 421 6 0 1 6.5 C[N+]1(Cc2ccccc2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140095 105982 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 421 6 0 1 6.5 C[N+]1(Cc2ccccc2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11431874 73933 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023763 73933 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
145958111 161466 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)CN 10.1021/acsmedchemlett.7b00406
CHEMBL4159607 161466 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)CN 10.1021/acsmedchemlett.7b00406
71463136 83521 0 None 2 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 12 4 5 5.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCCC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206608 83521 0 None 2 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 12 4 5 5.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCCC2)cc1 10.1016/j.bmcl.2012.09.085
76320690 105979 0 None -1 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085063 105979 0 None -1 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140092 105979 0 None -1 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
6908726 108478 5 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Agonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contractionAgonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contraction
ChEMBL 274 3 1 5 2.2 O=C(N/N=C/c1ccsc1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2018.07.015
CHEMBL3211778 108478 5 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Agonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contractionAgonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contraction
ChEMBL 274 3 1 5 2.2 O=C(N/N=C/c1ccsc1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2018.07.015
42626096 12636 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1ccc(C(O)(c2ccc(OC)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187802 12636 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1ccc(C(O)(c2ccc(OC)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL521921 12636 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1ccc(C(O)(c2ccc(OC)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
137647734 157304 0 None -2 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4083681 157304 0 None -2 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
44234683 106022 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1ccc(F)cc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cc(F)ccc1C 10.1021/jm900736e
CHEMBL3084406 106022 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1ccc(F)cc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cc(F)ccc1C 10.1021/jm900736e
CHEMBL3140205 106022 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1ccc(F)cc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cc(F)ccc1C 10.1021/jm900736e
46830361 7809 0 None -10 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 433 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3c(F)c(F)c(F)c(F)c3F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090094 7809 0 None -10 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 433 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3c(F)c(F)c(F)c(F)c3F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
137637944 155274 0 None -3 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4059829 155274 0 None -3 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
11364984 186678 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 2 6 3.2 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)n2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL492701 186678 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 2 6 3.2 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)n2)CCN1 10.1016/j.bmcl.2009.01.098
44590169 187660 0 None -7 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 603 11 3 7 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL499565 187660 0 None -7 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 603 11 3 7 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL539885 187660 0 None -7 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 603 11 3 7 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
11606547 12492 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 484 8 1 2 6.4 CC(C)(C)c1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1186941 12492 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 484 8 1 2 6.4 CC(C)(C)c1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL483253 12492 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 484 8 1 2 6.4 CC(C)(C)c1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
71463134 83510 0 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 618 11 3 6 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N(C)Cc2n(C)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206594 83510 0 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 618 11 3 6 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N(C)Cc2n(C)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
44589574 172119 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 582 11 4 6 3.9 CCN(CC)C(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450093 172119 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 582 11 4 6 3.9 CCN(CC)C(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44573543 186906 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.01.098
CHEMBL494151 186906 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.01.098
11399125 192550 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 471 6 1 5 3.7 CC(=O)N1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL523012 192550 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 471 6 1 5 3.7 CC(=O)N1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
11619198 106009 0 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 365 4 0 2 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085058 106009 0 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 365 4 0 2 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140170 106009 0 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 365 4 0 2 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
137655063 158427 0 None -3 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096143 158427 0 None -3 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
76313454 106025 0 None 1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085064 106025 0 None 1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140214 106025 0 None 1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
122195453 123591 0 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633663 123591 0 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
71450662 83592 0 None -1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 611 13 4 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2207176 83592 0 None -1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 611 13 4 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
122195446 123590 0 None -1 5 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
CHEMBL3633656 123590 0 None -1 5 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
76324334 105995 0 None -2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 369 4 0 3 4.5 Cc1ccoc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085070 105995 0 None -2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 369 4 0 3 4.5 Cc1ccoc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3140112 105995 0 None -2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 369 4 0 3 4.5 Cc1ccoc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
46830362 7812 0 None -8 5 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090097 7812 0 None -8 5 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
76327902 103024 0 None -1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 354 4 0 4 4.4 Cc1ccoc1CN(C(=O)O[C@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085088 103024 0 None -1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 354 4 0 4 4.4 Cc1ccoc1CN(C(=O)O[C@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
46883796 7811 0 None -1 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 411 4 1 3 4.8 CCN1CCN(c2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090096 7811 0 None -1 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 411 4 1 3 4.8 CCN1CCN(c2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
71463135 83520 0 None 2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 607 12 4 5 5.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206607 83520 0 None 2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 607 12 4 5 5.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCC2)cc1 10.1016/j.bmcl.2012.09.085
71455968 83512 0 None 2 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206599 83512 0 None 2 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
11168935 186780 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493329 186780 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
44589496 185399 0 None 15 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 10 5 7 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL486983 185399 0 None 15 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 10 5 7 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076445 212670 0 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5081816 212998 0 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
11215075 186754 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493131 186754 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
11410490 187016 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494741 187016 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
11249473 187099 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL495172 187099 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44590175 188047 0 None -3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 3 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL503025 188047 0 None -3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 3 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553433 188047 0 None -3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 3 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590035 191158 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3OC)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL519760 191158 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3OC)C2)cc1 10.1016/j.bmcl.2008.09.020
152278786 182170 0 None -30 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 182170 0 None -30 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
71452455 83505 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 565 9 3 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(CC3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206588 83505 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 565 9 3 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(CC3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
44573305 186679 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 449 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)s2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL492702 186679 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 449 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)s2)CCN1 10.1016/j.bmcl.2009.01.098
11398832 187028 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 1 5 3.8 CN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL494781 187028 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 1 5 3.8 CN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44573620 187052 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 469 7 2 4 4.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494953 187052 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 469 7 2 4 4.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
44573499 187136 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL495360 187136 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
44573466 192709 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL524168 192709 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
44589569 172163 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 11 5 6 3.5 CCCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450685 172163 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 11 5 6 3.5 CCCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589572 188398 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 602 10 5 6 4.6 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)Nc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL508556 188398 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 602 10 5 6 4.6 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)Nc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
162657046 180261 0 None -79 4 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@H](C)C1 10.1021/acsmedchemlett.0c00626
CHEMBL4757103 180261 0 None -79 4 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@H](C)C1 10.1021/acsmedchemlett.0c00626
44573786 186726 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 5 2 5 3.1 O=C(NCc1cccc(-c2cccc(C(=O)N3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL492989 186726 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 5 2 5 3.1 O=C(NCc1cccc(-c2cccc(C(=O)N3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
71454215 83511 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 714 13 4 6 6.5 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCc2n(Cc3ccc(Cl)cc3)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206595 83511 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 714 13 4 6 6.5 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCc2n(Cc3ccc(Cl)cc3)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
122195454 123593 0 None -8 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633665 123593 0 None -8 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
122195453 123591 0 None -2 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633663 123591 0 None -2 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
10092649 192471 51 None -69 11 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 192471 51 None -69 11 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
10092649 192471 51 None -69 11 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 192471 51 None -69 11 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
152278786 182170 0 None -30 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 182170 0 None -30 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
76327900 106001 0 None -1 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085061 106001 0 None -1 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140142 106001 0 None -1 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
3156646 8180 9 None -6 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1092460 8180 9 None -6 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
76309757 103023 0 None 1 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 340 4 0 4 4.0 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085087 103023 0 None 1 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 340 4 0 4 4.0 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
122195446 123590 0 None -1 5 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
CHEMBL3633656 123590 0 None -1 5 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
71454217 83514 0 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 551 9 3 5 4.3 CC[N+]1(C2CCN(C(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)CC2)CCCC1 10.1016/j.bmcl.2012.09.085
CHEMBL2206601 83514 0 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 551 9 3 5 4.3 CC[N+]1(C2CCN(C(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)CC2)CCCC1 10.1016/j.bmcl.2012.09.085
122195454 123593 0 None -8 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633665 123593 0 None -8 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
71450616 83519 0 None 2 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 591 11 4 5 4.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)C23CC4CC(CC(C4)C2)C3)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206606 83519 0 None 2 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 591 11 4 5 4.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)C23CC4CC(CC(C4)C2)C3)cc1 10.1016/j.bmcl.2012.09.085
11284402 192113 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1ccc(F)c(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL521986 192113 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1ccc(F)c(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44589583 171914 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 561 10 5 6 3.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL448294 171914 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 561 10 5 6 3.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555471 171914 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 561 10 5 6 3.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590168 172160 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450652 172160 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540399 172160 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44589584 188193 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 563 10 4 5 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL505651 188193 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 563 10 4 5 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540144 188193 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 563 10 4 5 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590122 191961 0 None 15 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 555 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C#N)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL521244 191961 0 None 15 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 555 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C#N)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
11626847 105994 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085068 105994 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3140111 105994 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
137655938 158438 0 None -64 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 362 6 2 4 3.0 NC/C=C\CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4096305 158438 0 None -64 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 362 6 2 4 3.0 NC/C=C\CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL5081816 212998 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44573785 186724 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 6 1 5 4.2 CN1CCCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL492987 186724 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 6 1 5 4.2 CN1CCCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44573544 192636 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL523712 192636 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2009.01.098
44573421 187027 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 5 3.7 O=C(Nc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494779 187027 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 5 3.7 O=C(Nc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573745 187067 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 6 1 4 5.0 O=C(NCc1cccc(-c2cccc(CN3CCCCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494997 187067 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 6 1 4 5.0 O=C(NCc1cccc(-c2cccc(CN3CCCCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
58975257 102902 0 None -1 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 377 6 2 2 3.9 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(N)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084638 102902 0 None -1 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 377 6 2 2 3.9 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(N)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
57758619 106010 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 499 15 0 1 9.2 CCCCCCCCCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084469 106010 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 499 15 0 1 9.2 CCCCCCCCCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140171 106010 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 499 15 0 1 9.2 CCCCCCCCCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44232706 105985 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1c(F)cccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cccc(F)c1C 10.1021/jm900736e
CHEMBL3084405 105985 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1c(F)cccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cccc(F)c1C 10.1021/jm900736e
CHEMBL3140098 105985 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1c(F)cccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cccc(F)c1C 10.1021/jm900736e
44234686 105997 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 4 1 3 5.1 Cc1cc(C(O)(C[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2csc(C)c2)cs1 10.1021/jm900736e
CHEMBL3084412 105997 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 4 1 3 5.1 Cc1cc(C(O)(C[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2csc(C)c2)cs1 10.1021/jm900736e
CHEMBL3140114 105997 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 4 1 3 5.1 Cc1cc(C(O)(C[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2csc(C)c2)cs1 10.1021/jm900736e
137654353 158470 0 None -1 6 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096589 158470 0 None -1 6 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
71457770 83513 0 None 1 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 647 10 3 5 6.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC([N+]3(Cc4ccc(Cl)cc4)CCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206600 83513 0 None 1 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 647 10 3 5 6.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC([N+]3(Cc4ccc(Cl)cc4)CCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
44233189 102926 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084678 102926 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233189 102926 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084678 102926 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
11602980 103027 0 None 1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 5 4.6 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085091 103027 0 None 1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 5 4.6 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
44590178 172169 0 None -1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450781 172169 0 None -1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540400 172169 0 None -1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590123 183278 0 None 15 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 564 10 4 6 4.3 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(Cl)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480877 183278 0 None 15 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 564 10 4 6 4.3 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(Cl)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
71457771 83515 0 None 5 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 691 14 4 5 7.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc(Cl)cc2)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206602 83515 0 None 5 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 691 14 4 5 7.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc(Cl)cc2)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
52176747 158485 1 None -16 8 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4096727 158485 1 None -16 8 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
2986945 94612 7 None -63 5 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 371 6 1 3 4.1 CCN1CCN(c2ccc(NC(=O)CCc3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255169 94612 7 None -63 5 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 371 6 1 3 4.1 CCN1CCN(c2ccc(NC(=O)CCc3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
76320692 106026 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 390 4 0 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085065 106026 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 390 4 0 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140215 106026 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 390 4 0 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
76309755 103014 0 None 1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085079 103014 0 None 1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44234681 106011 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C2 10.1021/jm900736e
CHEMBL3084404 106011 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C2 10.1021/jm900736e
CHEMBL3140172 106011 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C2 10.1021/jm900736e
76316970 103011 0 None 2 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 350 4 0 3 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085076 103011 0 None 2 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 350 4 0 3 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
145960175 161579 0 None -27 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(\F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4161528 161579 0 None -27 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(\F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
76313457 103016 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085080 103016 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
137638270 156335 0 None -6 5 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4071900 156335 0 None -6 5 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
44573465 186691 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL492802 186691 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
11410317 186725 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 441 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3C[C@@H]4C[C@H]3CN4)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL492988 186725 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 441 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3C[C@@H]4C[C@H]3CN4)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
11443944 187101 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL495180 187101 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL5076535 212674 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44573545 187017 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 403 6 2 3 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(F)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494742 187017 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 403 6 2 3 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(F)c1 10.1016/j.bmcl.2009.01.098
44590166 188827 0 None 3 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 468 9 4 6 2.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL513228 188827 0 None 3 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 468 9 4 6 2.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC)C2)cc1 10.1016/j.bmcl.2008.09.020
44573422 187055 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 3 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494962 187055 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 3 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
71459691 83518 0 None -5 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 723 14 4 5 8.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc3ccccc3c2)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206605 83518 0 None -5 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 723 14 4 5 8.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc3ccccc3c2)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
1090202 8406 11 None 1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 377 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3ccccc3Cl)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1094003 8406 11 None 1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 377 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3ccccc3Cl)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
44233928 85647 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2308786 85647 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233928 85647 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2308786 85647 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
57758624 105983 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084467 105983 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140096 105983 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11691471 12460 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 398 6 1 1 5.2 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1186783 12460 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 398 6 1 1 5.2 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL478070 12460 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 398 6 1 1 5.2 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCc3ccccc3)(CC1)CC2 10.1021/jm801601v
145951963 162452 0 None -199 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(/F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4175500 162452 0 None -199 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(/F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
11398062 105981 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 427 6 0 1 6.9 C[N+]1(CC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084464 105981 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 427 6 0 1 6.9 C[N+]1(CC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140094 105981 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 427 6 0 1 6.9 C[N+]1(CC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11692150 12521 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187107 12521 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL490651 12521 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
145950432 162402 0 None -120 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)=C(\F)CN 10.1021/acsmedchemlett.7b00406
CHEMBL4174727 162402 0 None -120 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)=C(\F)CN 10.1021/acsmedchemlett.7b00406
76313456 106027 0 None -1 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
CHEMBL3085066 106027 0 None -1 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
CHEMBL3140216 106027 0 None -1 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
66875589 102915 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084662 102915 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11504490 192003 0 None - 0 Human 11.0 pKd = 11 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL521523 192003 0 None - 0 Human 11.0 pKd = 11 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
11504490 192003 0 None - 0 Human 11.0 pKd = 11 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL521523 192003 0 None - 0 Human 11.0 pKd = 11 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
25034186 199753 0 None - 0 Human 10.9 pKd = 10.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 722 11 4 8 7.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC4CCCCC4)s3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL540396 199753 0 None - 0 Human 10.9 pKd = 10.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 722 11 4 8 7.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC4CCCCC4)s3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL604842 199753 0 None - 0 Human 10.9 pKd = 10.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 722 11 4 8 7.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC4CCCCC4)s3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
25195533 77983 1 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2103803 77983 1 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2110584 77983 1 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
25195533 77983 1 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2103803 77983 1 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2110584 77983 1 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
44589580 172577 0 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 635 10 5 7 5.3 C[N+]1(Cc2ccc(O)cc2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC3CCCCC3)s2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL452142 172577 0 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 635 10 5 7 5.3 C[N+]1(Cc2ccc(O)cc2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC3CCCCC3)s2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL553448 172577 0 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 635 10 5 7 5.3 C[N+]1(Cc2ccc(O)cc2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC3CCCCC3)s2)C1 10.1016/j.bmcl.2008.09.020
11533795 12509 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(F)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187076 12509 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(F)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL489212 12509 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(F)c3)(CC1)CC2 10.1021/jm801601v
25034184 187813 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 676 11 4 7 6.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL501803 187813 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 676 11 4 7 6.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL539887 187813 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 676 11 4 7 6.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
11442669 74106 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023760 74106 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2027876 74106 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11519069 3876 2 None - 0 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11519070 3876 2 None - 0 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
4816 3876 2 None - 0 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
7354 3876 2 None - 0 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
CHEMBL1187833 3876 2 None - 0 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
DB09076 3876 2 None - 0 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11528123 192032 0 None - 0 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 529 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL521696 192032 0 None - 0 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 529 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
42626090 12508 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187075 12508 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL489211 12508 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
42626094 12516 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3F)(CC1)CC2 10.1021/jm801601v
CHEMBL1187092 12516 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3F)(CC1)CC2 10.1021/jm801601v
CHEMBL490237 12516 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3F)(CC1)CC2 10.1021/jm801601v
11585117 12652 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Br)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187851 12652 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Br)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL523957 12652 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Br)cc3)(CC1)CC2 10.1021/jm801601v
70689729 74130 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 479 10 0 2 6.9 C[N+]1(CCCOCc2ccccc2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2021997 74130 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 479 10 0 2 6.9 C[N+]1(CCCOCc2ccccc2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2028006 74130 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 479 10 0 2 6.9 C[N+]1(CCCOCc2ccccc2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11753447 186768 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 459 7 2 4 4.4 CC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
CHEMBL493265 186768 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 459 7 2 4 4.4 CC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
11365314 186769 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 473 8 2 4 4.8 CCC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
CHEMBL493266 186769 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 473 8 2 4 4.8 CCC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
57758618 105991 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 359 5 0 1 5.3 CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084457 105991 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 359 5 0 1 5.3 CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140108 105991 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 359 5 0 1 5.3 CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
57758626 106007 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 373 6 0 1 5.7 CCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084458 106007 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 373 6 0 1 5.7 CCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140168 106007 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 373 6 0 1 5.7 CCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
57758627 106008 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084459 106008 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140169 106008 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44232952 102908 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084650 102908 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
11592005 12638 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1ccc(F)cc1)(c1ccc(F)cc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187807 12638 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1ccc(F)cc1)(c1ccc(F)cc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL522081 12638 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1ccc(F)cc1)(c1ccc(F)cc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
11649606 12644 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 462 8 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Cl)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187835 12644 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 462 8 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Cl)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL523474 12644 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 462 8 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Cl)cc3)(CC1)CC2 10.1021/jm801601v
11651006 188361 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 573 11 3 6 3.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(CCCO)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL508097 188361 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 573 11 3 6 3.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(CCCO)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11519318 12635 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(F)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187800 12635 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(F)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL521781 12635 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(F)cc3)(CC1)CC2 10.1021/jm801601v
11693689 170361 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 620 10 2 4 5.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(Cc6ccccc6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL445527 170361 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 620 10 2 4 5.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(Cc6ccccc6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL554706 170361 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 620 10 2 4 5.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(Cc6ccccc6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
44573747 187134 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 9 2 5 3.5 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C=O)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL495350 187134 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 9 2 5 3.5 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C=O)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
70685520 74116 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 443 11 0 1 7.6 CCCCCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2021998 74116 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 443 11 0 1 7.6 CCCCCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2027937 74116 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 443 11 0 1 7.6 CCCCCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44233188 102779 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 5 1 2 3.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084419 102779 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 5 1 2 3.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44234688 105998 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 346 3 0 0 5.8 Cc1ccccc1C(=C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084414 105998 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 346 3 0 0 5.8 Cc1ccccc1C(=C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140115 105998 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 346 3 0 0 5.8 Cc1ccccc1C(=C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
11223598 106043 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084413 106043 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140264 106043 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
42626019 12458 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL1186756 12458 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL476434 12458 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
25195533 77983 1 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2103803 77983 1 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2110584 77983 1 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11586041 172115 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 572 10 2 4 4.9 CCC[N+]1(C)CCN(Cc2cccc(C(=O)NCc3ccc(F)c(-c4cccc(CN5CCN[C@@H](C)C5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL450060 172115 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 572 10 2 4 4.9 CCC[N+]1(C)CCN(Cc2cccc(C(=O)NCc3ccc(F)c(-c4cccc(CN5CCN[C@@H](C)C5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL540251 172115 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 572 10 2 4 4.9 CCC[N+]1(C)CCN(Cc2cccc(C(=O)NCc3ccc(F)c(-c4cccc(CN5CCN[C@@H](C)C5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44589581 188202 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 615 12 5 6 4.9 C=CC[N+]1(Cc2cccc(O)c2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC(C)C)cc2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL505751 188202 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 615 12 5 6 4.9 C=CC[N+]1(Cc2cccc(O)c2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC(C)C)cc2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL540145 188202 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 615 12 5 6 4.9 C=CC[N+]1(Cc2cccc(O)c2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC(C)C)cc2)C1 10.1016/j.bmcl.2008.09.020
44589579 188467 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 595 10 5 7 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)s1 10.1016/j.bmcl.2008.09.020
CHEMBL509515 188467 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 595 10 5 7 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)s1 10.1016/j.bmcl.2008.09.020
CHEMBL540148 188467 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 595 10 5 7 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)s1 10.1016/j.bmcl.2008.09.020
44233930 106042 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 363 5 1 1 3.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084409 106042 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 363 5 1 1 3.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140263 106042 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 363 5 1 1 3.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
42626017 12654 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(Br)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187854 12654 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(Br)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL524119 12654 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(Br)c3)(CC1)CC2 10.1021/jm801601v
25034182 172015 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL448870 172015 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL540359 172015 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
11585987 187135 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 516 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCOCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL495358 187135 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 516 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCOCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11607628 187728 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 584 8 2 4 5.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+]6(CCCCC6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL500560 187728 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 584 8 2 4 5.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+]6(CCCCC6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL539886 187728 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 584 8 2 4 5.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+]6(CCCCC6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
25034182 172015 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL448870 172015 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540359 172015 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
25132856 186633 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL492437 186633 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
25132856 186633 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL492437 186633 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11556983 186782 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493331 186782 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL538864 186782 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL555476 186782 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
57758616 105992 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 398 7 0 2 5.6 C[N+]1(CCCC#N)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084463 105992 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 398 7 0 2 5.6 C[N+]1(CCCC#N)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140109 105992 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 398 7 0 2 5.6 C[N+]1(CCCC#N)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
57758629 106014 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 375 6 1 2 4.3 C[N+]1(CCO)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084460 106014 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 375 6 1 2 4.3 C[N+]1(CCO)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140180 106014 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 375 6 1 2 4.3 C[N+]1(CCO)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11535362 187035 0 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 545 12 2 5 4.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)CCCN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL494837 187035 0 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 545 12 2 5 4.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)CCCN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
16086059 80363 0 None - 0 Rat 9.7 pKd = 9.7 Functional
Antagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat tracheaAntagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat trachea
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215180 80363 0 None - 0 Rat 9.7 pKd = 9.7 Functional
Antagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat tracheaAntagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat trachea
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
11249888 186794 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 442 6 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C#N)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL493465 186794 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 442 6 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C#N)c4)ccc3F)c2)CCN1 10.1021/jm800935u
11642407 12511 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1cccc(F)c1)(c1cccc(F)c1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187079 12511 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1cccc(F)c1)(c1cccc(F)c1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL489625 12511 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1cccc(F)c1)(c1cccc(F)c1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
11564285 192552 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 8 2 5 4.4 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL523044 192552 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 8 2 5 4.4 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
44232952 102908 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084650 102908 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11519069 3876 2 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11519070 3876 2 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
4816 3876 2 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
7354 3876 2 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
CHEMBL1187833 3876 2 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
DB09076 3876 2 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
42625938 12507 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 337 5 2 2 2.9 NCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187073 12507 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 337 5 2 2 2.9 NCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL489032 12507 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 337 5 2 2 2.9 NCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
15951517 12518 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 8 1 2 4.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL1187094 12518 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 8 1 2 4.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL490243 12518 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 8 1 2 4.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
11512119 12645 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 453 8 1 3 5.0 N#Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187838 12645 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 453 8 1 3 5.0 N#Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL523598 12645 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 453 8 1 3 5.0 N#Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
69058946 105993 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084658 105993 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140110 105993 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
69058946 105993 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084658 105993 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3140110 105993 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
42625944 12497 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 426 8 1 1 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1186964 12497 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 426 8 1 1 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL484475 12497 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 426 8 1 1 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCc3ccccc3)(CC1)CC2 10.1021/jm801601v
16041939 12519 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 423 8 0 2 5.3 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL1187095 12519 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 423 8 0 2 5.3 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL490244 12519 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 423 8 0 2 5.3 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
57758617 105980 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 389 7 0 2 4.9 COCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084462 105980 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 389 7 0 2 4.9 COCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140093 105980 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 389 7 0 2 4.9 COCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11636578 192475 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 2 4 5.2 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL522495 192475 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 2 4 5.2 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
44589582 171075 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 12 4 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](CC3CC3)(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL446587 171075 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 12 4 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](CC3CC3)(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL550885 171075 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 12 4 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](CC3CC3)(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589576 188469 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 6 5 3.9 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL509520 188469 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 6 5 3.9 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555706 188469 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 6 5 3.9 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
57758613 106018 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 433 10 0 3 4.9 COCCOCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084468 106018 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 433 10 0 3 4.9 COCCOCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140184 106018 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 433 10 0 3 4.9 COCCOCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11705920 12640 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 7 1 2 5.0 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187810 12640 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 7 1 2 5.0 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL522418 12640 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 7 1 2 5.0 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
11633226 106046 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 344 3 0 2 5.6 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084418 106046 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 344 3 0 2 5.6 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140267 106046 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 344 3 0 2 5.6 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11223598 106043 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084413 106043 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140264 106043 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11691950 12653 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187853 12653 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL524097 12653 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
57758623 106016 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 371 6 0 1 5.5 C=CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084461 106016 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 371 6 0 1 5.5 C=CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140182 106016 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 371 6 0 1 5.5 C=CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44234690 106045 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 4 1 1 4.7 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084417 106045 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 4 1 1 4.7 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140266 106045 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 4 1 1 4.7 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44232949 106044 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 362 4 1 3 4.8 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084415 106044 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 362 4 1 3 4.8 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140265 106044 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 362 4 1 3 4.8 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11635210 12627 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 458 9 1 3 5.1 COc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL1187765 12627 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 458 9 1 3 5.1 COc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL519652 12627 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 458 9 1 3 5.1 COc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
44589578 172599 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1nc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)no1 10.1016/j.bmcl.2008.09.020
CHEMBL452193 172599 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1nc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)no1 10.1016/j.bmcl.2008.09.020
CHEMBL540401 172599 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1nc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)no1 10.1016/j.bmcl.2008.09.020
44589577 188381 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1noc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)n1 10.1016/j.bmcl.2008.09.020
CHEMBL508343 188381 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1noc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)n1 10.1016/j.bmcl.2008.09.020
CHEMBL540146 188381 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1noc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)n1 10.1016/j.bmcl.2008.09.020
44232702 106021 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3084401 106021 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3140203 106021 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
11692150 12521 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187107 12521 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL490651 12521 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
25034182 172015 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL448870 172015 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL540359 172015 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
76327869 102776 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 333 4 1 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084396 102776 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 333 4 1 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
66875589 102915 0 None - 1 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084662 102915 0 None - 1 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11235700 105986 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084410 105986 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140099 105986 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
66875589 102915 0 None - 1 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084662 102915 0 None - 1 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
44233192 106000 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084643 106000 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3140141 106000 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
42626088 12515 0 None - 1 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL1187091 12515 0 None - 1 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL490236 12515 0 None - 1 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
42626013 12517 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 437 8 0 2 5.7 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187093 12517 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 437 8 0 2 5.7 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL490242 12517 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 437 8 0 2 5.7 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
11722039 186781 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 530 8 3 4 3.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C[N+]5(C)CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493330 186781 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 530 8 3 4 3.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C[N+]5(C)CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL558605 186781 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 530 8 3 4 3.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C[N+]5(C)CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11650778 186889 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 474 8 2 4 4.3 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL494022 186889 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 474 8 2 4 4.3 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
16042745 184719 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 551 8 4 5 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+]3(CCCCCC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL485932 184719 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 551 8 4 5 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+]3(CCCCCC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL538360 184719 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 551 8 4 5 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+]3(CCCCCC3)C2)cc1 10.1016/j.bmcl.2008.09.020
44233190 102927 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084679 102927 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233192 106000 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084643 106000 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140141 106000 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233190 102927 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084679 102927 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
42626092 12526 0 None - 1 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187132 12526 0 None - 1 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL491246 12526 0 None - 1 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
66604762 106028 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 318 3 0 0 5.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084398 106028 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 318 3 0 0 5.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140217 106028 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 318 3 0 0 5.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44232700 106029 0 None - 1 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084399 106029 0 None - 1 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140218 106029 0 None - 1 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
16065402 67585 0 None - 0 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 428 9 1 3 4.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910848 67585 0 None - 0 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 428 9 1 3 4.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2)C1 10.1021/jm200884j
367 3764 8 None -10 5 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
5487427 3764 8 None -10 5 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
8592 3764 8 None -10 5 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL1900528 3764 8 None -10 5 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL3305968 3764 8 None -10 5 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL4650755 3764 8 None -10 5 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
DB01409 3764 8 None -10 5 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
54757541 67589 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2O)C1 10.1021/jm200884j
CHEMBL1910852 67589 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2O)C1 10.1021/jm200884j
54757856 67594 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 10 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(OCc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910857 67594 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 10 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(OCc2cccc(O)c2)C1 10.1021/jm200884j
25897919 55363 11 None 1 3 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
657309 55363 11 None 1 3 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1464005 55363 11 None 1 3 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1621597 55363 11 None 1 3 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
16065403 67593 16 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910856 67593 16 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
16034837 67588 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910851 67588 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
16065543 67599 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(Cl)c2)C1 10.1021/jm200884j
CHEMBL1910862 67599 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(Cl)c2)C1 10.1021/jm200884j
16065135 67583 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910846 67583 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2)C1 10.1021/jm200884j
16065407 67602 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2F)C1 10.1021/jm200884j
CHEMBL1910865 67602 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2F)C1 10.1021/jm200884j
16065268 67586 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 456 9 1 3 5.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2ccccc2)CC1 10.1021/jm200884j
CHEMBL1910849 67586 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 456 9 1 3 5.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2ccccc2)CC1 10.1021/jm200884j
16065137 67587 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910850 67587 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
54757544 67597 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 476 9 2 4 5.0 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
CHEMBL1910860 67597 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 476 9 2 4 5.0 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
16065405 67600 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
CHEMBL1910863 67600 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
16065541 67603 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)ccc2F)C1 10.1021/jm200884j
CHEMBL1910866 67603 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)ccc2F)C1 10.1021/jm200884j
16065406 67595 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 470 9 2 4 5.0 NC(=O)C(CCC1(N2CC(Oc3cccc(O)c3)C2)CCCC1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
CHEMBL1910858 67595 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 470 9 2 4 5.0 NC(=O)C(CCC1(N2CC(Oc3cccc(O)c3)C2)CCCC1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
54757543 67590 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(O)cc2)C1 10.1021/jm200884j
CHEMBL1910853 67590 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(O)cc2)C1 10.1021/jm200884j
16065136 67584 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910847 67584 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2ccccc2)C1 10.1021/jm200884j
16065404 67598 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
CHEMBL1910861 67598 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
126534204 137903 0 None - 0 Human 6.0 pKi = 6.0 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
CHEMBL3774411 137903 0 None - 0 Human 6.0 pKi = 6.0 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
54757653 67592 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2O)C1 10.1021/jm200884j
CHEMBL1910855 67592 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2O)C1 10.1021/jm200884j
121304590 144825 0 None - 0 Human 5.9 pKi = 5.9 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3913607 144825 0 None - 0 Human 5.9 pKi = 5.9 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121304477 151639 0 None - 0 Human 5.9 pKi = 5.9 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 487 7 0 6 5.6 Cc1ncccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3968272 151639 0 None - 0 Human 5.9 pKi = 5.9 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 487 7 0 6 5.6 Cc1ncccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
126534771 138064 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 424 7 0 8 3.5 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccccc4)C3C2)n1C 10.1016/j.bmc.2016.02.031
CHEMBL3775589 138064 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 424 7 0 8 3.5 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccccc4)C3C2)n1C 10.1016/j.bmc.2016.02.031
126533969 137939 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 427 7 0 7 3.4 Cn1c(SCCCN2CC3CCN(c4ccccc4)C3C2)nnc1C1CCOCC1 10.1016/j.bmc.2016.02.031
CHEMBL3774649 137939 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 427 7 0 7 3.4 Cn1c(SCCCN2CC3CCN(c4ccccc4)C3C2)nnc1C1CCOCC1 10.1016/j.bmc.2016.02.031
121304609 152428 0 None - 0 Human 5.8 pKi = 5.8 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3975147 152428 0 None - 0 Human 5.8 pKi = 5.8 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
121304654 148345 0 None - 0 Human 6.7 pKi = 6.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 530 8 1 7 4.7 Cc1nc(C(N)=O)ccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3941520 148345 0 None - 0 Human 6.7 pKi = 6.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 530 8 1 7 4.7 Cc1nc(C(N)=O)ccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121304538 149473 0 None - 0 Human 6.7 pKi = 6.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 516 8 1 7 4.4 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)nc1 10.1021/acs.jmedchem.6b00972
CHEMBL3950254 149473 0 None - 0 Human 6.7 pKi = 6.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 516 8 1 7 4.4 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)nc1 10.1021/acs.jmedchem.6b00972
54757542 67596 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 492 9 2 4 5.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
CHEMBL1910859 67596 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 492 9 2 4 5.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
16065269 67591 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 472 9 2 4 5.3 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2cccc(O)c2)CC1 10.1021/jm200884j
CHEMBL1910854 67591 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 472 9 2 4 5.3 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2cccc(O)c2)CC1 10.1021/jm200884j
54757332 67582 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 414 9 1 3 4.4 NC(=O)C(CCCN1CC[C@H](Oc2ccccc2)C1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
CHEMBL1910845 67582 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 414 9 1 3 4.4 NC(=O)C(CCCN1CC[C@H](Oc2ccccc2)C1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
121304458 153455 0 None - 0 Human 5.7 pKi = 5.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 409 7 0 7 4.1 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccccc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3983937 153455 0 None - 0 Human 5.7 pKi = 5.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 409 7 0 7 4.1 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccccc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121304867 153665 0 None - 0 Human 5.7 pKi = 5.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3985877 153665 0 None - 0 Human 5.7 pKi = 5.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
126534291 138012 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 488 7 0 7 4.6 Cn1c(SCCCN2CC3CCN(c4ccccc4C(F)(F)F)C3C2)nnc1-c1cccnc1 10.1016/j.bmc.2016.02.031
CHEMBL3775197 138012 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 488 7 0 7 4.6 Cn1c(SCCCN2CC3CCN(c4ccccc4C(F)(F)F)C3C2)nnc1-c1cccnc1 10.1016/j.bmc.2016.02.031
121304598 144713 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 535 8 1 6 5.4 CC(=O)NC1CCC(c2nnc(SCCCN3CC[C@]4(C[C@@H]4c4ccc(C(F)(F)F)cc4)C3)n2C)CC1 10.1021/acs.jmedchem.6b00972
CHEMBL3912801 144713 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 535 8 1 6 5.4 CC(=O)NC1CCC(c2nnc(SCCCN3CC[C@]4(C[C@@H]4c4ccc(C(F)(F)F)cc4)C3)n2C)CC1 10.1021/acs.jmedchem.6b00972
126534373 138017 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 510 7 0 8 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4F)C3C2)n1C 10.1016/j.bmc.2016.02.031
CHEMBL3775226 138017 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 510 7 0 8 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4F)C3C2)n1C 10.1016/j.bmc.2016.02.031
121304464 143812 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 8 4.7 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1csnn1 10.1021/acs.jmedchem.6b00972
CHEMBL3905582 143812 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 8 4.7 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1csnn1 10.1021/acs.jmedchem.6b00972
121304485 147643 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3935692 147643 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
10125445 75675 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at muscarinic M3 receptorAntagonist activity at muscarinic M3 receptor
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1021/jm800582j
CHEMBL205654 75675 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at muscarinic M3 receptorAntagonist activity at muscarinic M3 receptor
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1021/jm800582j
121304452 148386 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(-c2ncco2)cc1 10.1021/acs.jmedchem.6b00972
CHEMBL3941818 148386 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(-c2ncco2)cc1 10.1021/acs.jmedchem.6b00972
121304574 142501 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 503 7 0 7 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccn(C)c(=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3894853 142501 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 503 7 0 7 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccn(C)c(=O)c1 10.1021/acs.jmedchem.6b00972
121304441 151852 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3970323 151852 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
121304408 143022 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)cc1 10.1021/acs.jmedchem.6b00972
CHEMBL3899125 143022 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)cc1 10.1021/acs.jmedchem.6b00972
121304649 150112 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3955505 150112 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
126535075 137950 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 518 7 0 8 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1ccc(=O)n(C)c1 10.1016/j.bmc.2016.02.031
CHEMBL3774769 137950 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 518 7 0 8 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1ccc(=O)n(C)c1 10.1016/j.bmc.2016.02.031
121304424 143312 0 None - 0 Human 6.3 pKi = 6.3 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3901587 143312 0 None - 0 Human 6.3 pKi = 6.3 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
134150754 151197 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CCC(=O)N=C1 10.1021/acs.jmedchem.6b00972
CHEMBL3964512 151197 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CCC(=O)N=C1 10.1021/acs.jmedchem.6b00972
134134147 142842 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CC=NC(=O)C1 10.1021/acs.jmedchem.6b00972
CHEMBL3897772 142842 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CC=NC(=O)C1 10.1021/acs.jmedchem.6b00972
134150637 151033 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 522 7 1 6 4.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCN(C(N)=O)CC1 10.1021/acs.jmedchem.6b00972
CHEMBL3963243 151033 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 522 7 1 6 4.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCN(C(N)=O)CC1 10.1021/acs.jmedchem.6b00972
54757766 67601 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 512 9 2 4 5.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)c(Cl)cc2Cl)C1 10.1021/jm200884j
CHEMBL1910864 67601 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 512 9 2 4 5.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)c(Cl)cc2Cl)C1 10.1021/jm200884j
483747 104930 2 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 503 4 0 5 4.9 Cc1ncnc(C)c1C(=O)N1CCC(C)(N2CCN([C@@H](C)c3ccc(C(F)(F)F)cc3)[C@@H](C)C2)CC1 10.1021/jm0304515
CHEMBL311795 104930 2 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 503 4 0 5 4.9 Cc1ncnc(C)c1C(=O)N1CCC(C)(N2CCN([C@@H](C)c3ccc(C(F)(F)F)cc3)[C@@H](C)C2)CC1 10.1021/jm0304515
121304500 149222 0 None - 0 Human 6.1 pKi = 6.1 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 6 5.1 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCOCC1 10.1021/acs.jmedchem.6b00972
CHEMBL3948167 149222 0 None - 0 Human 6.1 pKi = 6.1 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 6 5.1 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCOCC1 10.1021/acs.jmedchem.6b00972
3009352 96191 1 None - 0 Human 5.0 pKi = 5.0 Functional
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 517 5 0 5 5.3 CC[C@@H](c1ccc(C(F)(F)F)cc1)N1CCN(C2(C)CCN(C(=O)c3c(C)ncnc3C)CC2)C[C@@H]1C 10.1021/jm0304515
CHEMBL263555 96191 1 None - 0 Human 5.0 pKi = 5.0 Functional
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 517 5 0 5 5.3 CC[C@@H](c1ccc(C(F)(F)F)cc1)N1CCN(C2(C)CCN(C(=O)c3c(C)ncnc3C)CC2)C[C@@H]1C 10.1021/jm0304515
316 2793 14 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
317 2793 14 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
71183 2793 14 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL3140030 2793 14 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL376897 2793 14 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
DB00462 2793 14 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
1979 76973 66 None -1 7 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 76973 66 None -1 7 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
187 253 34 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 253 34 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 253 34 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 253 34 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 253 34 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 253 34 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
1726 2461 12 None 2 6 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1993 2461 12 None 2 6 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
7438 2461 12 None 2 6 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
CHEMBL978 2461 12 None 2 6 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
DB06709 2461 12 None 2 6 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
2166 3074 46 None 1 8 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
305 3074 46 None 1 8 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
5910 3074 46 None 1 8 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
CHEMBL550 3074 46 None 1 8 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
DB01085 3074 46 None 1 8 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
123603 870 25 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
2684 870 25 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
584 870 25 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
9658 870 25 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
CHEMBL168815 870 25 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
5831 214185 0 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
3008304 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 19438238
7632 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 19438238
CHEMBL523685 3960 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 19438238
1726 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1726 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
1993 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1993 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
7438 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
7438 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
CHEMBL978 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
CHEMBL978 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
DB06709 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
DB06709 2461 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
288 249 0 None -3 5 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
6979053 249 0 None -3 5 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
286 250 0 None -3 5 Human 5.7 pEC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
6954180 250 0 None -3 5 Human 5.7 pEC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
20824 215965 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 378 5 3 5 0.5 CC1(C)S[C@@H]2[C@H](NC(=O)C(C(O)=O)C3=CC=CC=C3)C(=O)N2[C@H]1C(O)=O None
18381 215975 0 None -1 4 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 469 4 2 6 3.2 CC1=C(C(=O)N[C@H]2[C@H]3SC(C)(C)[C@@H](N3C2=O)C(O)=O)C(=NO1)C1=C(Cl)C=CC=C1Cl None
11693 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
11693 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
3494 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
3494 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
4302 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
4302 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
7459 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
7459 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
CHEMBL1201335 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
CHEMBL1201335 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
DB00986 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
DB00986 1797 12 None -1 5 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
154059 3580 49 None -1 3 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
2457 3580 49 None -1 3 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
7483 3580 49 None -1 3 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
CHEMBL1734 3580 49 None -1 3 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
DB01591 3580 49 None -1 3 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
6433090 216025 0 None -1 2 Human 8.0 pKb = 8.0 Functional
NoneNone
Drug Central 319 6 1 3 3.1 CC1=NC=CN1CCC(C(N)=O)(C1=CC=CC=C1)C1=CC=CC=C1 None


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
316 2793 14 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
317 2793 14 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
71183 2793 14 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL3140030 2793 14 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL376897 2793 14 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
DB00462 2793 14 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
316 2793 14 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
317 2793 14 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
71183 2793 14 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL3140030 2793 14 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL376897 2793 14 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
DB00462 2793 14 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
367 3764 8 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
5487427 3764 8 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
8592 3764 8 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL1900528 3764 8 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL3305968 3764 8 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL4650755 3764 8 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
DB01409 3764 8 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
2230 461 55 None -588 10 Human 7.0 pEC50 = 7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
296 461 55 None -588 10 Human 7.0 pEC50 = 7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
CHEMBL7303 461 55 None -588 10 Human 7.0 pEC50 = 7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
DB04365 461 55 None -588 10 Human 7.0 pEC50 = 7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
9308 17572 16 None - 7 Human 6.0 pEC50 = 6 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL1255785 17572 16 None - 7 Human 6.0 pEC50 = 6 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL12587 17572 16 None - 7 Human 6.0 pEC50 = 6 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL292911 17572 16 None - 7 Human 6.0 pEC50 = 6 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
170332 160429 1 None -7 3 Human 5.0 pEC50 = 5 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 160429 1 None -7 3 Human 5.0 pEC50 = 5 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 160429 1 None -7 3 Human 5.0 pEC50 = 5 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
170332 160429 1 None -7 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 160429 1 None -7 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 160429 1 None -7 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
319 1297 39 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1297 39 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1297 39 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1297 39 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1297 39 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1297 39 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
13621561 10967 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 178 2 1 4 0.3 C#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177918 10967 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 178 2 1 4 0.3 C#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL6767 10967 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 178 2 1 4 0.3 C#CCOc1noc2c1CNCC2 10.1021/jm00156a018
10261985 202251 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69306 202251 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
13621555 11839 3 None - 0 Human 4.9 pEC50 = 4.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 180 3 1 4 0.9 C=CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1182820 11839 3 None - 0 Human 4.9 pEC50 = 4.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 180 3 1 4 0.9 C=CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL268175 11839 3 None - 0 Human 4.9 pEC50 = 4.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 180 3 1 4 0.9 C=CCOc1noc2c1CNCC2 10.1021/jm00156a018
10465280 102312 1 None - 0 Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL305264 102312 1 None - 0 Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2 10.1021/jm00012a019
13621569 11848 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCOc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL1182850 11848 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCOc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL269706 11848 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCOc1noc2c1CN(C)CC2 10.1021/jm00156a018
303 2930 16 None -89 6 Human 5.8 pEC50 = 5.8 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
4629 2930 16 None -89 6 Human 5.8 pEC50 = 5.8 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
8595 2930 16 None -89 6 Human 5.8 pEC50 = 5.8 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL44674 2930 16 None -89 6 Human 5.8 pEC50 = 5.8 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
125603 10962 9 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 154 1 1 4 0.3 COc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177907 10962 9 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 154 1 1 4 0.3 COc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL6451 10962 9 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 154 1 1 4 0.3 COc1noc2c1CNCC2 10.1021/jm00156a018
2551 782 23 None -346 11 Human 5.8 pEC50 = 5.8 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
298 782 23 None -346 11 Human 5.8 pEC50 = 5.8 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
488 782 23 None -346 11 Human 5.8 pEC50 = 5.8 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
CHEMBL965 782 23 None -346 11 Human 5.8 pEC50 = 5.8 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
DB00411 782 23 None -346 11 Human 5.8 pEC50 = 5.8 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
2551 782 23 None -346 11 Human 5.7 pEC50 = 5.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
298 782 23 None -346 11 Human 5.7 pEC50 = 5.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
488 782 23 None -346 11 Human 5.7 pEC50 = 5.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL965 782 23 None -346 11 Human 5.7 pEC50 = 5.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
DB00411 782 23 None -346 11 Human 5.7 pEC50 = 5.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
156009673 177679 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4633816 177679 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650683 177679 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156014812 177687 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4647437 177687 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650736 177687 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
13621572 10964 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCN1CCc2onc(OC)c2C1 10.1021/jm00156a018
CHEMBL1177910 10964 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCN1CCc2onc(OC)c2C1 10.1021/jm00156a018
CHEMBL6568 10964 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCN1CCc2onc(OC)c2C1 10.1021/jm00156a018
302 2929 23 None -309 7 Human 6.7 pEC50 = 6.7 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
4630 2929 23 None -309 7 Human 6.7 pEC50 = 6.7 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
CHEMBL7634 2929 23 None -309 7 Human 6.7 pEC50 = 6.7 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
2551 782 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
298 782 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
488 782 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
CHEMBL965 782 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
DB00411 782 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
187 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187 253 34 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
294 253 34 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
65 253 34 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
8593 253 34 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL667 253 34 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
DB03128 253 34 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
187 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 253 34 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 253 34 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
156015097 176978 0 None 1 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4640324 176978 0 None 1 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
156015300 177018 0 None 4 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177018 0 None 4 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
156021744 177540 0 None 1 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4648071 177540 0 None 1 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
160492 96808 32 None - 0 Human 6.5 pEC50 = 6.5 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 141 1 1 3 0.1 COC(=O)C1=CCCNC1 10.1021/jm00156a018
CHEMBL268808 96808 32 None - 0 Human 6.5 pEC50 = 6.5 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 141 1 1 3 0.1 COC(=O)C1=CCCNC1 10.1021/jm00156a018
2230 461 55 None -588 10 Human 6.5 pEC50 = 6.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
296 461 55 None -588 10 Human 6.5 pEC50 = 6.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
CHEMBL7303 461 55 None -588 10 Human 6.5 pEC50 = 6.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
DB04365 461 55 None -588 10 Human 6.5 pEC50 = 6.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
13621545 10965 4 None - 0 Human 5.5 pEC50 = 5.5 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 2 1 4 0.7 CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177913 10965 4 None - 0 Human 5.5 pEC50 = 5.5 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 2 1 4 0.7 CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL6680 10965 4 None - 0 Human 5.5 pEC50 = 5.5 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 2 1 4 0.7 CCOc1noc2c1CNCC2 10.1021/jm00156a018
137629935 160473 0 None -1 3 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 160473 0 None -1 3 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 160473 0 None -1 3 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
156011965 176718 0 None 3 3 Human 8.4 pEC50 = 8.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 176718 0 None 3 3 Human 8.4 pEC50 = 8.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
13621565 10971 1 None - 0 Human 5.4 pEC50 = 5.4 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 192 2 1 4 0.7 CC#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177927 10971 1 None - 0 Human 5.4 pEC50 = 5.4 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 192 2 1 4 0.7 CC#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL7018 10971 1 None - 0 Human 5.4 pEC50 = 5.4 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 192 2 1 4 0.7 CC#CCOc1noc2c1CNCC2 10.1021/jm00156a018
10442337 202250 2 None - 0 Human 6.3 pEC50 = 6.3 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69305 202250 2 None - 0 Human 6.3 pEC50 = 6.3 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
10442081 102135 9 None - 0 Human 6.2 pEC50 = 6.2 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL304142 102135 9 None - 0 Human 6.2 pEC50 = 6.2 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
3008304 3960 48 None - 0 Human 5.2 pEC50 = 5.2 Binding
Positive allosteric modulation activity at muscarinic M3 receptorPositive allosteric modulation activity at muscarinic M3 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
7632 3960 48 None - 0 Human 5.2 pEC50 = 5.2 Binding
Positive allosteric modulation activity at muscarinic M3 receptorPositive allosteric modulation activity at muscarinic M3 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
CHEMBL523685 3960 48 None - 0 Human 5.2 pEC50 = 5.2 Binding
Positive allosteric modulation activity at muscarinic M3 receptorPositive allosteric modulation activity at muscarinic M3 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
2551 782 23 None -346 11 Human 7.2 pEC50 = 7.2 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
298 782 23 None -346 11 Human 7.2 pEC50 = 7.2 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
488 782 23 None -346 11 Human 7.2 pEC50 = 7.2 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
CHEMBL965 782 23 None -346 11 Human 7.2 pEC50 = 7.2 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
DB00411 782 23 None -346 11 Human 7.2 pEC50 = 7.2 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
13621567 97708 7 None - 0 Human 6.1 pEC50 = 6.1 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 1 0 4 0.7 COc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL27384 97708 7 None - 0 Human 6.1 pEC50 = 6.1 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 1 0 4 0.7 COc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL440085 97708 7 None - 0 Human 6.1 pEC50 = 6.1 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 1 0 4 0.7 COc1noc2c1CN(C)CC2 10.1021/jm00156a018
57400422 71287 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 330 4 0 2 3.9 C[C@@](C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924027 71287 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 330 4 0 2 3.9 C[C@@](C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1963462 71287 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 330 4 0 2 3.9 C[C@@](C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
24758141 103252 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 4 0 2 3.9 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087959 103252 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 4 0 2 3.9 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2013.09.092
367 3764 8 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
5487427 3764 8 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
8592 3764 8 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
CHEMBL1900528 3764 8 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
CHEMBL3305968 3764 8 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
CHEMBL4650755 3764 8 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
DB01409 3764 8 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
57392578 68405 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 487 7 0 4 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(Cl)s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921908 68405 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 487 7 0 4 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(Cl)s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395222 68806 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924040 68806 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545528 103160 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 453 7 0 4 5.5 O=C(O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087230 103160 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 453 7 0 4 5.5 O=C(O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545784 103164 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 475 7 0 4 6.1 O=C(O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087235 103164 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 475 7 0 4 6.1 O=C(O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
57401273 68404 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 525 7 0 3 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cccc(Br)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921907 68404 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 525 7 0 3 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cccc(Br)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57394170 68419 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 517 8 0 4 6.4 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cc4ccccc4s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921925 68419 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 517 8 0 4 6.4 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cc4ccccc4s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57394234 68429 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 483 9 0 5 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921935 68429 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 483 9 0 5 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
59179619 103254 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 327 3 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)C1(c2ccccc2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087961 103254 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 327 3 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)C1(c2ccccc2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545282 103261 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 440 6 0 3 6.0 Cc1ccc(CC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)s1 10.1016/j.bmcl.2013.09.092
CHEMBL3088081 103261 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 440 6 0 3 6.0 Cc1ccc(CC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)s1 10.1016/j.bmcl.2013.09.092
72545526 103265 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.8 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088086 103265 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.8 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
57390665 68411 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921917 68411 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395990 68431 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 9 0 5 5.2 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921937 68431 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 9 0 5 5.2 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546493 103250 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087957 103250 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
58348375 103255 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 333 3 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088075 103255 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 333 3 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545281 103260 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 420 6 0 2 5.6 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088080 103260 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 420 6 0 2 5.6 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
57395991 68439 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 1 5 4.4 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921945 68439 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 1 5 4.4 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57391636 68494 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 7 1 7 3.7 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cncc(Cl)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922053 68494 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 7 1 7 3.7 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cncc(Cl)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988645 68802 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 351 4 0 4 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924036 68802 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 351 4 0 4 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546026 103170 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 439 6 2 4 3.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cc[nH]n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087242 103170 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 439 6 2 4 3.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cc[nH]n1 10.1016/j.bmcl.2013.09.092
72543916 103242 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncc(Cl)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087949 103242 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncc(Cl)n1 10.1016/j.bmcl.2013.09.092
72546261 103245 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 447 5 0 4 5.7 O=C(O[C@H]1C[N+]2(Cc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087952 103245 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 447 5 0 4 5.7 O=C(O[C@H]1C[N+]2(Cc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
11434515 259 3 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
11519741 259 3 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
4484 259 3 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
7449 259 3 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
CHEMBL1194325 259 3 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
DB08897 259 3 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
44552684 68413 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1cc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)ccn1 10.1016/j.bmcl.2011.10.002
CHEMBL1921919 68413 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1cc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)ccn1 10.1016/j.bmcl.2011.10.002
57397792 68435 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 406 6 1 5 2.1 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921941 68435 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 406 6 1 5 2.1 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57401219 68440 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 7 1 5 3.6 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921946 68440 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 7 1 5 3.6 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57391775 68813 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924049 68813 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
11693 1797 12 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
3494 1797 12 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
4302 1797 12 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
7459 1797 12 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
CHEMBL1201335 1797 12 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
DB00986 1797 12 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
72545787 103167 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 467 6 1 3 5.1 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccc(F)c1 10.1016/j.bmcl.2013.09.092
CHEMBL3087238 103167 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 467 6 1 3 5.1 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccc(F)c1 10.1016/j.bmcl.2013.09.092
72545525 103264 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.6 O=C(O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088085 103264 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.6 O=C(O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
44517831 68403 2 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921904 68403 2 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395952 68407 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 7 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3=CC4CCOC4C=C3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921911 68407 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 7 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3=CC4CCOC4C=C3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397744 68412 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 468 8 0 5 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921918 68412 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 468 8 0 5 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57390720 68492 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 467 7 1 6 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922051 68492 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 467 7 1 6 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57403853 68495 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 488 6 0 5 5.2 Cc1ccc2nc(C[N+]34CCC(CC3)[C@@H](OC(=O)[C@](C)(c3ccccc3)N3CCCCC3)C4)oc2c1 10.1016/j.bmcl.2011.10.002
CHEMBL1922054 68495 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 488 6 0 5 5.2 Cc1ccc2nc(C[N+]34CCC(CC3)[C@@H](OC(=O)[C@](C)(c3ccccc3)N3CCCCC3)C4)oc2c1 10.1016/j.bmcl.2011.10.002
57398751 68793 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 471 7 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924025 68793 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 471 7 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545530 103161 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 7 0 3 5.7 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087232 103161 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 7 0 3 5.7 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
72546025 103169 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 454 6 1 5 4.3 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)no1 10.1016/j.bmcl.2013.09.092
CHEMBL3087241 103169 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 454 6 1 5 4.3 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)no1 10.1016/j.bmcl.2013.09.092
72546496 103183 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087362 103183 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccn1 10.1016/j.bmcl.2013.09.092
72546739 103188 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccncn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087367 103188 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccncn1 10.1016/j.bmcl.2013.09.092
72546991 103189 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087368 103189 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnn1 10.1016/j.bmcl.2013.09.092
72546262 103246 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087953 103246 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545285 103263 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 436 7 0 3 5.4 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088084 103263 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 436 7 0 3 5.4 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
11434515 259 3 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
11519741 259 3 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
4484 259 3 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
7449 259 3 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
CHEMBL1194325 259 3 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
DB08897 259 3 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
10143956 13798 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL1196359 13798 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL556635 13798 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
57390766 68406 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 7 0 3 5.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc4ccccc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921910 68406 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 7 0 3 5.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc4ccccc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57402931 68410 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 459 7 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3CCCCC3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921914 68410 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 459 7 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3CCCCC3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57399407 68421 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 475 9 0 3 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921927 68421 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 475 9 0 3 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57401217 68434 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 400 6 1 4 2.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921940 68434 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 400 6 1 4 2.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397793 68436 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 7 1 4 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921942 68436 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 7 1 4 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57401218 68437 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 482 7 1 5 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921943 68437 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 482 7 1 5 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397794 68438 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 494 7 1 4 4.3 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921944 68438 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 494 7 1 4 4.3 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57392520 68491 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cnccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922050 68491 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cnccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57392521 68493 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 473 7 1 7 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922052 68493 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 473 7 1 7 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395096 68496 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 0 5 5.4 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922055 68496 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 0 5 5.4 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545785 103165 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 373 5 1 3 2.9 NC(=O)C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2 10.1016/j.bmcl.2013.09.092
CHEMBL3087236 103165 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 373 5 1 3 2.9 NC(=O)C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2 10.1016/j.bmcl.2013.09.092
72546736 103185 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087364 103185 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnc1 10.1016/j.bmcl.2013.09.092
72547500 103239 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(Cl)nn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087946 103239 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(Cl)nn1 10.1016/j.bmcl.2013.09.092
10165877 62800 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779133 62800 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789396 62800 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
11852298 13912 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1197251 13912 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL564057 13912 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
71524764 143907 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 833 16 5 14 6.5 COc1cc(-c2noc(CCCN(C)[C@H]3CC[C@H](OC(=O)C(O)(c4cccs4)c4cccs4)CC3)n2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3906438 143907 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 833 16 5 14 6.5 COc1cc(-c2noc(CCCN(C)[C@H]3CC[C@H](OC(=O)C(O)(c4cccs4)c4cccs4)CC3)n2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
54592025 147462 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 695 18 5 10 6.4 CN(CCCCCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3934254 147462 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 695 18 5 10 6.4 CN(CCCCCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
44232927 193667 7 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 349 4 1 6 2.7 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL551729 193667 7 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 349 4 1 6 2.7 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
86765983 145281 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 342 4 0 2 4.1 C[C@@](C(=O)O[C@@H]1CC2CCC1[N+]2(C)C)(c1ccccc1)C1CCCC1 nan
CHEMBL3917058 145281 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 342 4 0 2 4.1 C[C@@](C(=O)O[C@@H]1CC2CCC1[N+]2(C)C)(c1ccccc1)C1CCCC1 nan
44233401 13513 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 10.1021/jm900132z
CHEMBL1194321 13513 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 10.1021/jm900132z
CHEMBL551327 13513 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 10.1021/jm900132z
44233177 13787 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1196246 13787 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL556221 13787 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 10.1021/jm900132z
44233403 13788 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL1196247 13788 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL556222 13788 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
53372934 128778 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670826 128778 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
53372936 128779 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670827 128779 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
11693 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
3494 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
4302 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
7459 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
CHEMBL1201335 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
DB00986 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
11693 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
3494 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
4302 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
7459 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
CHEMBL1201335 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
DB00986 1797 12 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
57392462 68422 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 481 9 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921928 68422 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 481 9 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57400294 68499 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 507 7 0 7 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3noc(-c4ccccc4)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922058 68499 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 507 7 0 7 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3noc(-c4ccccc4)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988644 68795 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 345 4 0 3 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924029 68795 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 345 4 0 3 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545786 103166 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 6 1 3 5.0 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087237 103166 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 6 1 3 5.0 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccc1 10.1016/j.bmcl.2013.09.092
72546993 103190 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncccc1F 10.1016/j.bmcl.2013.09.092
CHEMBL3087370 103190 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncccc1F 10.1016/j.bmcl.2013.09.092
72547254 103195 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 518 6 1 4 5.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(C(F)(F)F)nc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087375 103195 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 518 6 1 4 5.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(C(F)(F)F)nc1 10.1016/j.bmcl.2013.09.092
72546263 103247 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087954 103247 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
69167248 103253 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 3 0 2 4.1 C[N+]1(C)CCC(OC(=O)C2(c3ccccc3)CCCCCC2)CC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087960 103253 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 3 0 2 4.1 C[N+]1(C)CCC(OC(=O)C2(c3ccccc3)CCCCCC2)CC1 10.1016/j.bmcl.2013.09.092
44236101 13914 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1197261 13914 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL564515 13914 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
10208897 62797 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 455 8 0 2 6.1 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779049 62797 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 455 8 0 2 6.1 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789387 62797 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 455 8 0 2 6.1 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10143718 62804 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779131 62804 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789435 62804 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
71558563 143248 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 14 5 13 5.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3900995 143248 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 14 5 13 5.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54673357 145080 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 795 17 5 12 6.7 COc1cc(OCCCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3915601 145080 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 795 17 5 12 6.7 COc1cc(OCCCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
53372938 128780 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 128780 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
1734 116 8 None 1 12 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
307 116 8 None 1 12 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
CHEMBL168067 116 8 None 1 12 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
11569908 13888 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1197028 13888 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL559106 13888 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
44232930 195018 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL564747 195018 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
57399406 68415 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cccnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921921 68415 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cccnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397746 68418 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 502 8 0 5 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921924 68418 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 502 8 0 5 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57394233 68426 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1ccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cc1 10.1016/j.bmcl.2011.10.002
CHEMBL1921932 68426 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1ccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cc1 10.1016/j.bmcl.2011.10.002
57395097 68497 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 7 0 6 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922056 68497 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 7 0 6 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546494 103251 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nnc(-c4ccccc4)o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087958 103251 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nnc(-c4ccccc4)o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
367 3764 8 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
5487427 3764 8 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
8592 3764 8 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL1900528 3764 8 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL3305968 3764 8 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL4650755 3764 8 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
DB01409 3764 8 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
20735153 13512 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1194314 13512 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL551063 13512 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1021/jm900132z
11489419 13507 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 448 10 1 5 5.2 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL1194274 13507 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 448 10 1 5 5.2 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL549784 13507 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 448 10 1 5 5.2 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
44232931 194707 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL562642 194707 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
57390666 68420 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 8 0 5 5.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccc4ncsc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921926 68420 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 8 0 5 5.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccc4ncsc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57396866 68498 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 506 7 0 6 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922057 68498 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 506 7 0 6 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546028 103172 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 457 6 1 6 3.9 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncns1 10.1016/j.bmcl.2013.09.092
CHEMBL3087244 103172 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 457 6 1 6 3.9 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncns1 10.1016/j.bmcl.2013.09.092
72547256 103197 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1nccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087377 103197 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1nccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
72546264 103248 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 472 6 0 4 5.8 O=C(O[C@H]1C[N+]2(Cc3ccn(-c4ccccc4)n3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087955 103248 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 472 6 0 4 5.8 O=C(O[C@H]1C[N+]2(Cc3ccn(-c4ccccc4)n3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
367 3764 8 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
5487427 3764 8 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
8592 3764 8 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
CHEMBL1900528 3764 8 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
CHEMBL3305968 3764 8 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
CHEMBL4650755 3764 8 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
DB01409 3764 8 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
71556977 142012 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 769 15 5 13 5.9 CN(CCCc1nc(-c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)no1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3890898 142012 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 769 15 5 13 5.9 CN(CCCc1nc(-c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)no1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
71566009 143775 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 838 17 5 13 5.4 COc1cc(OCC(=O)N(C)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3905320 143775 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 838 17 5 13 5.4 COc1cc(OCC(=O)N(C)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
71558416 150795 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 757 14 6 12 4.9 CN(CCCn1c(=O)[nH]c2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3961014 150795 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 757 14 6 12 4.9 CN(CCCn1c(=O)[nH]c2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
121347973 151096 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 732 14 5 13 4.6 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4c3OCC(=O)N4)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
CHEMBL3963770 151096 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 732 14 5 13 4.6 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4c3OCC(=O)N4)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
1734 116 8 None 1 12 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
307 116 8 None 1 12 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
CHEMBL168067 116 8 None 1 12 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
1734 116 8 None 1 12 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
307 116 8 None 1 12 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
CHEMBL168067 116 8 None 1 12 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
44236098 193975 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL556426 193975 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
1734 116 8 None 1 12 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
307 116 8 None 1 12 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
CHEMBL168067 116 8 None 1 12 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
44236340 13680 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1195513 13680 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL554725 13680 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
44232685 13915 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL1197273 13915 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL564765 13915 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
10119939 62798 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1777827 62798 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789388 62798 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
71558718 144189 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 14 5 13 5.7 CN(CCCn1c(=O)sc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3908788 144189 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 14 5 13 5.7 CN(CCCn1c(=O)sc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
57392515 68433 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 10 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921939 68433 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 10 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545783 103163 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 438 7 0 4 4.7 Cn1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087234 103163 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 438 7 0 4 4.7 Cn1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
72546994 103191 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087371 103191 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nc1 10.1016/j.bmcl.2013.09.092
1734 116 8 None 1 12 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
307 116 8 None 1 12 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL168067 116 8 None 1 12 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
44232681 13901 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 0 5 5.7 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1197156 13901 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 0 5 5.7 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL561187 13901 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 0 5 5.7 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1 10.1021/jm900132z
1734 116 8 None 1 12 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
307 116 8 None 1 12 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
CHEMBL168067 116 8 None 1 12 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
9928017 62010 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779033 62010 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10229167 62795 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 427 9 0 3 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779136 62795 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 427 9 0 3 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789385 62795 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 427 9 0 3 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
10393952 62799 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 529 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779140 62799 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 529 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1789389 62799 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 529 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
10187216 62808 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 461 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779128 62808 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 461 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789452 62808 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 461 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10143858 62809 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779132 62809 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789454 62809 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
44236336 13899 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 364 4 1 5 2.8 C[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL1197131 13899 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 364 4 1 5 2.8 C[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL560327 13899 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 364 4 1 5 2.8 C[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
71558567 142149 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 740 14 5 11 6.2 CN(CCCn1ccc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3892021 142149 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 740 14 5 11 6.2 CN(CCCn1ccc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
121347950 150700 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 728 14 5 12 5.1 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
CHEMBL3960091 150700 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 728 14 5 12 5.1 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
44232683 13515 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
CHEMBL1194336 13515 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
CHEMBL551731 13515 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
57399408 68423 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 463 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921929 68423 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 463 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395989 68430 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 495 9 0 4 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921936 68430 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 495 9 0 4 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57391773 68812 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 425 7 0 3 4.9 CC(C)=CCC[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
CHEMBL1924046 68812 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 425 7 0 3 4.9 CC(C)=CCC[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
72546738 103187 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncnc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087366 103187 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncnc1 10.1016/j.bmcl.2013.09.092
72546995 103192 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(F)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087372 103192 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(F)cn1 10.1016/j.bmcl.2013.09.092
72543915 103241 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cncc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087948 103241 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cncc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
10007638 120363 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 8 2 4 4.4 O=C(N[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401648 120363 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 8 2 4 4.4 O=C(N[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559195 120363 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 8 2 4 4.4 O=C(N[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
67548926 120365 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 473 8 2 5 4.5 O=C(N[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401649 120365 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 473 8 2 5 4.5 O=C(N[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559201 120365 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 473 8 2 5 4.5 O=C(N[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
10325942 120366 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 8 2 5 3.9 O=C(N[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401650 120366 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 8 2 5 3.9 O=C(N[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559202 120366 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 8 2 5 3.9 O=C(N[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
44236099 193882 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL554699 193882 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
54673354 148194 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 808 16 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3940214 148194 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 808 16 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
44236332 13903 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL1197183 13903 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL561870 13903 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
72548703 161019 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161019 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
939077 193398 2 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 0 4 3.6 O=C(O[C@H]1CN2CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL549577 193398 2 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 0 4 3.6 O=C(O[C@H]1CN2CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
57397791 68432 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921938 68432 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57402222 68796 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 353 4 0 3 3.6 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1C=CC=CC=C1 10.1016/j.bmcl.2011.10.002
CHEMBL1924030 68796 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 353 4 0 3 3.6 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1C=CC=CC=C1 10.1016/j.bmcl.2011.10.002
57397002 68797 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 363 4 0 4 2.7 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCSCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924031 68797 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 363 4 0 4 2.7 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCSCC1 10.1016/j.bmcl.2011.10.002
72547252 103193 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c1 10.1016/j.bmcl.2013.09.092
CHEMBL3087373 103193 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c1 10.1016/j.bmcl.2013.09.092
72547255 103196 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087376 103196 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
72547498 103199 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087379 103199 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nn1 10.1016/j.bmcl.2013.09.092
72547501 103240 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087947 103240 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
11678378 120373 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 7 1 3 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
CHEMBL3401654 120373 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 7 1 3 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
CHEMBL3559211 120373 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 7 1 3 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
10164137 62796 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 423 9 0 3 5.1 CCCCN(C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779137 62796 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 423 9 0 3 5.1 CCCCN(C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789386 62796 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 423 9 0 3 5.1 CCCCN(C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
10300661 62807 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 421 9 0 2 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779135 62807 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 421 9 0 2 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789451 62807 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 421 9 0 2 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
117628769 144493 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 772 15 5 13 5.2 CN(CCCn1c(=O)oc2cc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3911114 144493 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 772 15 5 13 5.2 CN(CCCn1c(=O)oc2cc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54586745 62810 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 523 8 0 2 6.8 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCCc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779138 62810 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 523 8 0 2 6.8 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCCc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1789461 62810 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 523 8 0 2 6.8 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCCc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
688566 194210 21 None - 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 337 4 1 4 2.6 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
CHEMBL558910 194210 21 None - 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 337 4 1 4 2.6 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
44235871 194897 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 1 4 2.5 O=C(O[C@H]1CN2CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL563887 194897 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 1 4 2.5 O=C(O[C@H]1CN2CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
44236334 13898 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL1197117 13898 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL559931 13898 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 10.1021/jm900132z
9946010 62011 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779034 62011 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10208972 62802 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 457 8 0 3 5.5 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779129 62802 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 457 8 0 3 5.5 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789429 62802 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 457 8 0 3 5.5 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
57390714 68427 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1cccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)c1 10.1016/j.bmcl.2011.10.002
CHEMBL1921933 68427 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1cccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)c1 10.1016/j.bmcl.2011.10.002
57395997 68490 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccnn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922049 68490 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccnn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988641 68799 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 359 4 0 3 3.4 CC1CCN(C(C)(C(=O)OC2CC[N+](C)(C)CC2)c2ccccc2)CC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924033 68799 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 359 4 0 3 3.4 CC1CCN(C(C)(C(=O)OC2CC[N+](C)(C)CC2)c2ccccc2)CC1 10.1016/j.bmcl.2011.10.002
57403964 68808 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 385 5 0 3 3.9 CC(C)[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
CHEMBL1924042 68808 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 385 5 0 3 3.9 CC(C)[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
72545782 103162 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 463 7 0 3 6.0 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c(C)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087233 103162 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 463 7 0 3 6.0 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c(C)n1 10.1016/j.bmcl.2013.09.092
72547497 103198 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)ncn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087378 103198 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)ncn1 10.1016/j.bmcl.2013.09.092
71565927 146128 0 None - 0 Human 9.0 pIC50 = 9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 12 4 11 6.3 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C2(C)c3ccccc3Oc3ccccc32)CC1 nan
CHEMBL3923686 146128 0 None - 0 Human 9.0 pIC50 = 9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 12 4 11 6.3 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C2(C)c3ccccc3Oc3ccccc32)CC1 nan
54672858 150941 0 None - 0 Human 9.0 pIC50 = 9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 16 7 12 5.9 COc1cc(NC(=O)CCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3962171 150941 0 None - 0 Human 9.0 pIC50 = 9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 16 7 12 5.9 COc1cc(NC(=O)CCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
44233175 13905 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL1197209 13905 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL562655 13905 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
44233173 13906 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1197216 13906 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL562890 13906 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
316 2793 14 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
317 2793 14 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
71183 2793 14 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
CHEMBL3140030 2793 14 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
CHEMBL376897 2793 14 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
DB00462 2793 14 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
10246307 117275 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 4 2 4 2.3 O=C(N[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1016/j.bmcl.2015.02.065
CHEMBL3401643 117275 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 4 2 4 2.3 O=C(N[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1016/j.bmcl.2015.02.065
54590925 152779 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 15 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3978112 152779 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 15 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
49800047 14334 1 None -2 5 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
CHEMBL1201024 14334 1 None -2 5 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
CHEMBL1201268 14334 1 None -2 5 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
9967590 61812 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 336 4 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1777826 61812 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 336 4 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
54582845 62801 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 525 8 0 3 6.2 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCOc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779139 62801 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 525 8 0 3 6.2 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCOc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1789405 62801 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 525 8 0 3 6.2 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCOc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
50925542 18983 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4cccc(Cl)c4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289653 18983 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4cccc(Cl)c4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
57401170 68416 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cn1 10.1016/j.bmcl.2011.10.002
CHEMBL1921922 68416 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cn1 10.1016/j.bmcl.2011.10.002
57397790 68425 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 8 0 4 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccc(Cl)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921931 68425 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 8 0 4 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccc(Cl)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57402970 68489 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccncn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922048 68489 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccncn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988643 68798 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 381 4 0 3 3.4 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCC(F)(F)CC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924032 68798 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 381 4 0 3 3.4 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCC(F)(F)CC1 10.1016/j.bmcl.2011.10.002
1201549 590 22 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 590 22 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 590 22 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 590 22 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 590 22 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 590 22 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
54592027 143461 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 717 15 5 11 5.3 CN(CCOc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3902803 143461 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 717 15 5 11 5.3 CN(CCOc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54583840 62022 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 404 4 0 3 4.7 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2CN3CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779045 62022 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 404 4 0 3 4.7 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2CN3CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
118638354 145054 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 17 5 11 5.3 CN(CCN(C)[C@H]1CC[C@H](OC(C(=O)O)(c2cccs2)c2cccs2)CC1)C(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 nan
CHEMBL3915401 145054 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 17 5 11 5.3 CN(CCN(C)[C@H]1CC[C@H](OC(C(=O)O)(c2cccs2)c2cccs2)CC1)C(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 nan
54673189 148630 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 801 15 6 14 5.3 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(C#N)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3943564 148630 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 801 15 6 14 5.3 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(C#N)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
25147683 62023 32 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 408 4 0 3 4.5 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779046 62023 32 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 408 4 0 3 4.5 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
10372836 101925 34 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
CHEMBL3039518 101925 34 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
54591014 145237 3 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
CHEMBL3916700 145237 3 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
71558565 166883 5 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 742 14 5 13 5.0 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 10.1021/acs.jmedchem.8b01520
CHEMBL4297483 166883 5 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 742 14 5 13 5.0 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 10.1021/acs.jmedchem.8b01520
155531077 171054 2 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 669 10 4 10 4.4 CC(C)c1ncc(C(=O)N2CCOC3(CCN(Cc4ccc(F)c(CCNC[C@H](O)c5ccc(O)c6[nH]c(=O)sc56)c4)CC3)C2)s1 10.1021/acs.jmedchem.8b01520
CHEMBL4465556 171054 2 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 669 10 4 10 4.4 CC(C)c1ncc(C(=O)N2CCOC3(CCN(Cc4ccc(F)c(CCNC[C@H](O)c5ccc(O)c6[nH]c(=O)sc56)c4)CC3)C2)s1 10.1021/acs.jmedchem.8b01520
57397743 68409 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 486 7 1 3 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3c[nH]c4ccccc34)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921913 68409 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 486 7 1 3 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3c[nH]c4ccccc34)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57393499 71254 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 2 3.5 CC(C(=O)O[C@@H]1CC[N+](C)(C)C1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924026 71254 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 2 3.5 CC(C(=O)O[C@@H]1CC[N+](C)(C)C1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1963231 71254 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 2 3.5 CC(C(=O)O[C@@H]1CC[N+](C)(C)C1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
54591014 145237 3 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3916700 145237 3 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
54673020 151054 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 766 14 6 11 5.5 CN(CCC(=O)Nc1cc(F)c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1F)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3963417 151054 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 766 14 6 11 5.5 CN(CCC(=O)Nc1cc(F)c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1F)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
10143954 13508 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL1194286 13508 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL549986 13508 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
11306852 13911 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 434 8 1 3 5.0 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C1(O)c3ccccc3-c3ccccc31)C2 10.1021/jm900132z
CHEMBL1197250 13911 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 434 8 1 3 5.0 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C1(O)c3ccccc3-c3ccccc31)C2 10.1021/jm900132z
CHEMBL563996 13911 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 434 8 1 3 5.0 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C1(O)c3ccccc3-c3ccccc31)C2 10.1021/jm900132z
25897919 55363 11 None 1 8 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2015.02.065
657309 55363 11 None 1 8 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2015.02.065
CHEMBL1464005 55363 11 None 1 8 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2015.02.065
CHEMBL1621597 55363 11 None 1 8 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2015.02.065
9944783 62014 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 316 6 0 3 3.9 CCCCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779037 62014 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 316 6 0 3 3.9 CCCCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
54673702 149099 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 814 15 6 14 5.6 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2c1OCC(=O)N2 nan
CHEMBL3947244 149099 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 814 15 6 14 5.6 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2c1OCC(=O)N2 nan
1734 116 8 None 1 12 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2010.07.034
307 116 8 None 1 12 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2010.07.034
CHEMBL168067 116 8 None 1 12 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2010.07.034
46890906 6964 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 329 5 2 2 4.8 OC(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1084850 6964 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 329 5 2 2 4.8 OC(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
50925541 18966 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289545 18966 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
57393500 68800 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 305 4 0 3 2.2 CN(C)C(C)(C(=O)OC1CC[N+](C)(C)CC1)c1ccccc1 10.1016/j.bmcl.2011.10.002
CHEMBL1924034 68800 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 305 4 0 3 2.2 CN(C)C(C)(C(=O)OC1CC[N+](C)(C)CC1)c1ccccc1 10.1016/j.bmcl.2011.10.002
72546495 103182 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 496 6 1 5 5.3 CC(C)(C)c1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)no1 10.1016/j.bmcl.2013.09.092
CHEMBL3087361 103182 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 496 6 1 5 5.3 CC(C)(C)c1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)no1 10.1016/j.bmcl.2013.09.092
102514695 181256 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]N -methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells incubated for 90 mins by scintillation counting methodDisplacement of [3H]N -methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells incubated for 90 mins by scintillation counting method
ChEMBL 970 18 0 10 9.4 O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)C1CN(C(=O)c2ccc(COc3cccc(CN(C(=O)O[C@H]4CN5CCC4CC5)c4ccccc4)c3)cc2)C1 10.1021/acs.jmedchem.9b02170
CHEMBL4778407 181256 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]N -methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells incubated for 90 mins by scintillation counting methodDisplacement of [3H]N -methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells incubated for 90 mins by scintillation counting method
ChEMBL 970 18 0 10 9.4 O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)C1CN(C(=O)c2ccc(COc3cccc(CN(C(=O)O[C@H]4CN5CCC4CC5)c4ccccc4)c3)cc2)C1 10.1021/acs.jmedchem.9b02170
52947552 18915 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 404 4 1 5 2.9 O=C(c1ccc(CO)o1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289201 18915 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 404 4 1 5 2.9 O=C(c1ccc(CO)o1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
52942458 19051 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 382 3 0 2 4.9 O=C(c1ccccc1)N1CCC2(CCN(Cc3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2010.10.016
CHEMBL1290183 19051 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 382 3 0 2 4.9 O=C(c1ccccc1)N1CCC2(CCN(Cc3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2010.10.016
52947320 19052 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 362 3 0 2 4.5 Cc1cccc(CN2CCC3(CC2)CCN(C(=O)c2ccccc2)CC3)c1 10.1016/j.bmcl.2010.10.016
CHEMBL1290184 19052 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 362 3 0 2 4.5 Cc1cccc(CN2CCC3(CC2)CCN(C(=O)c2ccccc2)CC3)c1 10.1016/j.bmcl.2010.10.016
72546023 103168 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 443 5 0 4 3.2 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)N1CCOCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087239 103168 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 443 5 0 4 3.2 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)N1CCOCC1 10.1016/j.bmcl.2013.09.092
9974222 11816 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1182709 11816 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL262198 11816 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
13578551 100814 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCN(CC)CCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL296405 100814 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCN(CC)CCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578548 100892 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 393 4 1 5 2.7 CN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL296988 100892 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 393 4 1 5 2.7 CN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
10094518 100923 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(C)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL297224 100923 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(C)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
46871665 6517 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F 10.1016/j.bmcl.2010.04.128
CHEMBL1083108 6517 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F 10.1016/j.bmcl.2010.04.128
13578551 100814 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCN(CC)CCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL296405 100814 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCN(CC)CCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
13578548 100892 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 393 4 1 5 2.7 CN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL296988 100892 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 393 4 1 5 2.7 CN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
10094518 100923 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(C)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL297224 100923 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(C)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
107867 2927 48 None -12 10 Rat 5.0 pIC50 = 5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
309 2927 48 None -12 10 Rat 5.0 pIC50 = 5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
CHEMBL17045 2927 48 None -12 10 Rat 5.0 pIC50 = 5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
46891141 6484 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 374 5 2 2 4.5 CC[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083002 6484 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 374 5 2 2 4.5 CC[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46891142 6485 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 364 4 2 2 3.8 O=C(NC[C@H]1CCNC[C@H]1F)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083003 6485 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 364 4 2 2 3.8 O=C(NC[C@H]1CCNC[C@H]1F)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46891143 6558 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 396 4 2 2 4.7 O=C(NCC1=C(F)CNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
CHEMBL1083317 6558 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 396 4 2 2 4.7 O=C(NCC1=C(F)CNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
107867 2927 48 None -12 10 Rat 5.0 pIC50 = 5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
309 2927 48 None -12 10 Rat 5.0 pIC50 = 5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
CHEMBL17045 2927 48 None -12 10 Rat 5.0 pIC50 = 5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
14660293 52373 3 None - 0 Human 4.0 pIC50 = 4 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2 10.1021/jm9705216
CHEMBL15936 52373 3 None - 0 Human 4.0 pIC50 = 4 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2 10.1021/jm9705216
44302755 200989 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 408 4 1 6 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61494 200989 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 408 4 1 6 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
10020681 117280 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 4 2 5 2.3 O=C(N[C@@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401657 117280 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 4 2 5 2.3 O=C(N[C@@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
44302727 101448 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccc(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL300987 101448 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccc(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
10782462 12008 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1184068 12008 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL330999 12008 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
10592484 11330 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180314 11330 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL121476 11330 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
44233173 13906 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
CHEMBL1197216 13906 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
CHEMBL562890 13906 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
9996901 117274 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 4 1 4 3.2 O=C(N[C@H]1CN2CCC1CC2)C(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401642 117274 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 4 1 4 3.2 O=C(N[C@H]1CN2CCC1CC2)C(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
135494454 172186 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 785 25 5 11 6.7 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL450986 172186 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 785 25 5 11 6.7 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
24739886 187286 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 469 6 1 3 4.2 NC(=O)CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL496376 187286 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 469 6 1 3 4.2 NC(=O)CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
2230 461 55 None -588 10 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
296 461 55 None -588 10 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
CHEMBL7303 461 55 None -588 10 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
DB04365 461 55 None -588 10 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
10641009 11321 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180292 11321 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL120472 11321 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
72546260 103173 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 440 6 1 5 4.0 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncco1 10.1016/j.bmcl.2013.09.092
CHEMBL3087245 103173 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 440 6 1 5 4.0 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncco1 10.1016/j.bmcl.2013.09.092
46890907 6965 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 311 4 1 1 5.4 Clc1cccc(-c2ccccc2/C=C/CC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1084851 6965 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 311 4 1 1 5.4 Clc1cccc(-c2ccccc2/C=C/CC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
10511551 25627 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL135328 25627 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@@H]1CN2CC[C@H]1C2 10.1021/jm9702903
10666533 11327 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
CHEMBL1180310 11327 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
CHEMBL121299 11327 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
10593954 12965 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1190178 12965 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL540316 12965 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
52947553 18916 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 374 3 0 4 3.4 O=C(c1ccoc1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289202 18916 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 374 3 0 4 3.4 O=C(c1ccoc1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
52943696 19069 2 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 348 3 0 2 4.2 O=C(c1ccccc1)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
CHEMBL1290294 19069 2 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 348 3 0 2 4.2 O=C(c1ccccc1)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
46890962 6942 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.4 O=C(Cc1ccccc1-c1cccc(Cl)c1)NC1CCNCC1 10.1016/j.bmcl.2010.04.127
CHEMBL1084804 6942 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.4 O=C(Cc1ccccc1-c1cccc(Cl)c1)NC1CCNCC1 10.1016/j.bmcl.2010.04.127
237 203157 43 None 1 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 203157 43 None 1 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 203157 43 None 1 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 203157 43 None 1 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
46891022 6584 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 380 4 2 2 4.5 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2010.04.127
CHEMBL1083404 6584 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 380 4 2 2 4.5 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2010.04.127
46871666 6991 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1084993 6991 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
46891144 7191 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 364 4 2 2 4.0 O=C(NCC1(F)CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1085985 7191 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 364 4 2 2 4.0 O=C(NCC1(F)CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
656392 183218 2 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 255 5 1 4 1.4 CC[C@@H](C)[C@@H](O)C(=O)OC[C@H]1CCN2CCC[C@@H]12 10.1021/np049650x
CHEMBL480464 183218 2 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 255 5 1 4 1.4 CC[C@@H](C)[C@@H](O)C(=O)OC[C@H]1CCN2CCC[C@@H]12 10.1021/np049650x
44302879 201030 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 348 1 1 4 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61774 201030 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 348 1 1 4 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
20735153 13512 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 nan
CHEMBL1194314 13512 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 nan
CHEMBL551063 13512 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 nan
44233177 13787 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 nan
CHEMBL1196246 13787 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 nan
CHEMBL556221 13787 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 nan
127053831 145690 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 7 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL3920279 145690 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 7 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
67547662 120372 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 482 7 2 3 4.2 CN(CCC[N+]12CCC(CC1)[C@@H](NC(=O)C1(O)c3ccccc3-c3ccccc31)C2)c1ccccc1 10.1016/j.bmcl.2015.02.065
CHEMBL3401653 120372 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 482 7 2 3 4.2 CN(CCC[N+]12CCC(CC1)[C@@H](NC(=O)C1(O)c3ccccc3-c3ccccc31)C2)c1ccccc1 10.1016/j.bmcl.2015.02.065
CHEMBL3559210 120372 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 482 7 2 3 4.2 CN(CCC[N+]12CCC(CC1)[C@@H](NC(=O)C1(O)c3ccccc3-c3ccccc31)C2)c1ccccc1 10.1016/j.bmcl.2015.02.065
154059 3580 49 None -1 8 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
2457 3580 49 None -1 8 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
7483 3580 49 None -1 8 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
CHEMBL1734 3580 49 None -1 8 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
DB01591 3580 49 None -1 8 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
44333603 109159 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 390 5 1 3 4.8 Cc1cc(C(=O)c2ccccc2)ccc1NC(=O)CC1CCCN2CCCC[C@H]12 10.1016/s0960-894x(99)00528-4
CHEMBL322378 109159 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 390 5 1 3 4.8 Cc1cc(C(=O)c2ccccc2)ccc1NC(=O)CC1CCCN2CCCC[C@H]12 10.1016/s0960-894x(99)00528-4
10567372 12025 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12025 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12025 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12025 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
44236332 13903 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
CHEMBL1197183 13903 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
CHEMBL561870 13903 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
127053830 149212 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 450 5 0 2 5.8 CC1(C(=O)O[C@H]2C[N+]3(C/C=C/c4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 nan
CHEMBL3948099 149212 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 450 5 0 2 5.8 CC1(C(=O)O[C@H]2C[N+]3(C/C=C/c4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 nan
127053828 149221 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 444 7 1 4 4.4 O=C(O[C@H]1C[N+]2(C/C=C/c3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
CHEMBL3948162 149221 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 444 7 1 4 4.4 O=C(O[C@H]1C[N+]2(C/C=C/c3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
135 2496 38 None -22 57 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2496 38 None -22 57 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2496 38 None -22 57 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2496 38 None -22 57 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2496 38 None -22 57 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
2774 3807 92 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
5593 3807 92 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
7319 3807 92 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
CHEMBL1200604 3807 92 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB00809 3807 92 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB01199 3807 92 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
10761219 11326 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1180309 11326 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL121298 11326 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
441383 20133 54 None -6 17 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 20133 54 None -6 17 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
12488 1627 51 None -8 23 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1627 51 None -8 23 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1627 51 None -8 23 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1627 51 None -8 23 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
44302741 200968 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61412 200968 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
10569816 11354 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
CHEMBL1180367 11354 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
CHEMBL124173 11354 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
2750 202363 69 None -1 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 202363 69 None -1 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
2745 3800 39 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572 3800 39 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
66007 3800 39 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
7315 3800 39 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
CHEMBL1490 3800 39 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
DB00376 3800 39 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
118728610 117272 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 336 4 2 3 2.1 O=C(N[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2015.02.065
CHEMBL3401640 117272 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 336 4 2 3 2.1 O=C(N[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2015.02.065
9946632 62020 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 354 4 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)c1ccc(F)cc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779043 62020 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 354 4 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)c1ccc(F)cc1 10.1016/j.bmcl.2011.03.096
44232683 13515 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 nan
CHEMBL1194336 13515 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 nan
CHEMBL551731 13515 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 nan
52948443 18999 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 419 4 0 5 3.9 CCc1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289758 18999 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 419 4 0 5 3.9 CCc1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
52947254 19012 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289865 19012 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
13578554 171859 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 461 5 1 5 4.4 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCC1 10.1021/jm00128a008
CHEMBL44773 171859 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 461 5 1 5 4.4 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCC1 10.1021/jm00128a008
24750278 88994 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of M3 receptor (unknown origin)Inhibition of M3 receptor (unknown origin)
ChEMBL 450 6 1 9 1.7 CC(C)=CCn1c(N2CCC[C@H](N)C2)nc2c1c(=O)n(CC(=O)c1ccccc1)c(=O)n2C 10.1021/acs.jmedchem.6b00475
CHEMBL237067 88994 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of M3 receptor (unknown origin)Inhibition of M3 receptor (unknown origin)
ChEMBL 450 6 1 9 1.7 CC(C)=CCn1c(N2CCC[C@H](N)C2)nc2c1c(=O)n(CC(=O)c1ccccc1)c(=O)n2C 10.1021/acs.jmedchem.6b00475
13578554 171859 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 461 5 1 5 4.4 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCC1 10.1021/jm00048a014
CHEMBL44773 171859 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 461 5 1 5 4.4 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCC1 10.1021/jm00048a014
14075467 101010 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(Cl)ccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL297818 101010 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(Cl)ccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578552 159630 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 419 4 1 5 3.3 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCC2)c2ccccc21 10.1021/jm00128a008
CHEMBL410928 159630 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 419 4 1 5 3.3 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCC2)c2ccccc21 10.1021/jm00128a008
14590397 187114 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 407 5 1 5 3.1 CCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL49525 187114 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 407 5 1 5 3.1 CCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578555 176106 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity of compound for glandular Muscarinic acetylcholine receptor M3 in rat using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity of compound for glandular Muscarinic acetylcholine receptor M3 in rat using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 433 4 1 5 3.7 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCCC2)c2ccccc21 10.1021/jm00128a008
CHEMBL45983 176106 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity of compound for glandular Muscarinic acetylcholine receptor M3 in rat using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity of compound for glandular Muscarinic acetylcholine receptor M3 in rat using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 433 4 1 5 3.7 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCCC2)c2ccccc21 10.1021/jm00128a008
14075467 101010 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(Cl)ccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL297818 101010 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(Cl)ccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
13578552 159630 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 419 4 1 5 3.3 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCC2)c2ccccc21 10.1021/jm00048a014
CHEMBL410928 159630 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 419 4 1 5 3.3 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCC2)c2ccccc21 10.1021/jm00048a014
13578555 176106 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 433 4 1 5 3.7 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCCC2)c2ccccc21 10.1021/jm00048a014
CHEMBL45983 176106 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 433 4 1 5 3.7 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCCC2)c2ccccc21 10.1021/jm00048a014
14590397 187114 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 407 5 1 5 3.1 CCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL49525 187114 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 407 5 1 5 3.1 CCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
14590396 171975 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.9 CCN(CC)CC1CCCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL44838 171975 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.9 CCN(CC)CC1CCCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
14590396 171975 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.9 CCN(CC)CC1CCCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL44838 171975 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.9 CCN(CC)CC1CCCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
2274 3124 53 None -21 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3124 53 None -21 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3124 53 None -21 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3124 53 None -21 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3124 53 None -21 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44302901 100587 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 320 1 1 3 3.9 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)cc34)OC21 10.1016/s0960-894x(98)00351-5
CHEMBL294726 100587 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 320 1 1 3 3.9 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)cc34)OC21 10.1016/s0960-894x(98)00351-5
9905467 11331 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180316 11331 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL121520 11331 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
44190762 176306 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from muscarinic M3 receptorDisplacement of radioligand from muscarinic M3 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
CHEMBL461571 176306 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from muscarinic M3 receptorDisplacement of radioligand from muscarinic M3 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
4841 67089 3 None -3 5 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1889399 67089 3 None -3 5 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1909073 67089 3 None -3 5 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
52950036 18965 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 391 3 0 5 3.3 O=C(c1cscn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289544 18965 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 391 3 0 5 3.3 O=C(c1cscn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
57391772 68801 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 361 8 0 3 3.8 CCCN(CCC)C(C)(C(=O)OC1CC[N+](C)(C)CC1)c1ccccc1 10.1016/j.bmcl.2011.10.002
CHEMBL1924035 68801 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 361 8 0 3 3.8 CCCN(CCC)C(C)(C(=O)OC1CC[N+](C)(C)CC1)c1ccccc1 10.1016/j.bmcl.2011.10.002
127053832 150267 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 6 0 4 5.2 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL3956752 150267 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 6 0 4 5.2 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
66592494 151055 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 457 8 1 6 4.1 O=C(O[C@H]1C[N+]2(CCCn3cccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3963421 151055 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 457 8 1 6 4.1 O=C(O[C@H]1C[N+]2(CCCn3cccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
10082470 52437 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
CHEMBL15944 52437 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
CHEMBL308608 52437 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
10522336 14961 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.3 CCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL120972 14961 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.3 CCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
44302728 197036 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 422 4 1 6 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL58228 197036 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 422 4 1 6 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
10806268 12031 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1184139 12031 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL334245 12031 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
10664532 12006 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184064 12006 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL330892 12006 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
10518821 12021 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184108 12021 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL332645 12021 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
10611310 12017 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1184096 12017 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL332335 12017 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
9966959 62018 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 6 0 4 3.6 CCCCN(Cc1cccs1)C(=O)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
CHEMBL1779041 62018 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 6 0 4 3.6 CCCCN(Cc1cccs1)C(=O)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
11569926 62803 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 441 7 0 2 5.7 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779048 62803 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 441 7 0 2 5.7 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789434 62803 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 441 7 0 2 5.7 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
2801 161325 56 None -1 28 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161325 56 None -1 28 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161325 56 None -1 28 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
302 2929 23 None -309 7 Human 4.8 pIC50 = 4.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
4630 2929 23 None -309 7 Human 4.8 pIC50 = 4.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
CHEMBL7634 2929 23 None -309 7 Human 4.8 pIC50 = 4.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
4543 169982 36 None -3 29 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169982 36 None -3 29 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169982 36 None -3 29 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
67547652 117279 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 2 0 3 3.5 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.02.065
CHEMBL3401647 117279 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 2 0 3 3.5 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.02.065
4601 205020 29 None -1 17 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 205020 29 None -1 17 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 205020 29 None -1 17 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
28417 39799 48 None -1 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 39799 48 None -1 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
191 399 92 None -37 28 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 399 92 None -37 28 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 399 92 None -37 28 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 399 92 None -37 28 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 399 92 None -37 28 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
3198 203802 73 None -10 34 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203802 73 None -10 34 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203802 73 None -10 34 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
43815 186337 58 None -5 24 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL1708 186337 58 None -5 24 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL490 186337 58 None -5 24 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
54586743 62811 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 357 4 0 3 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2011.03.096
CHEMBL1779130 62811 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 357 4 0 3 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2011.03.096
CHEMBL1789462 62811 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 357 4 0 3 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2011.03.096
67549179 117277 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 2 2 3 2.1 O=C(N[C@H]1CN2CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1016/j.bmcl.2015.02.065
CHEMBL3401645 117277 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 2 2 3 2.1 O=C(N[C@H]1CN2CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1016/j.bmcl.2015.02.065
10808719 12026 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184120 12026 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL333125 12026 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
448537 159703 86 None -28 25 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159703 86 None -28 25 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
18456768 62805 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 407 8 0 2 5.3 CCCCN(C(=O)O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779134 62805 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 407 8 0 2 5.3 CCCCN(C(=O)O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789445 62805 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 407 8 0 2 5.3 CCCCN(C(=O)O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
53372934 128778 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670826 128778 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
66592724 147410 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 476 6 1 5 4.9 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
CHEMBL3933797 147410 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 476 6 1 5 4.9 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
52942401 19022 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4Cl)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289982 19022 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4Cl)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
46891020 6582 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 363 5 1 3 4.2 O=S(=O)(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083402 6582 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 363 5 1 3 4.2 O=S(=O)(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
15730 70774 73 None -1 10 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
CHEMBL195437 70774 73 None -1 10 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
6075 149575 36 None -3 16 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 149575 36 None -3 16 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
10829928 12296 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1 10.1021/jm980067l
CHEMBL1185758 12296 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1 10.1021/jm980067l
CHEMBL431688 12296 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1 10.1021/jm980067l
52946359 18931 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 3 0 6 2.7 O=C(c1cnsn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289314 18931 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 3 0 6 2.7 O=C(c1cnsn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
46890960 7108 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.6 O=C(NCc1ccccc1-c1cccc(Cl)c1)C1CCNCC1 10.1016/j.bmcl.2010.04.127
CHEMBL1085556 7108 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.6 O=C(NCc1ccccc1-c1cccc(Cl)c1)C1CCNCC1 10.1016/j.bmcl.2010.04.127
10053614 120367 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401651 120367 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559203 120367 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
54672859 147514 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 778 15 6 12 5.4 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(F)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3934681 147514 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 778 15 6 12 5.4 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(F)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
25897919 55363 11 None 1 8 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
657309 55363 11 None 1 8 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
CHEMBL1464005 55363 11 None 1 8 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
CHEMBL1621597 55363 11 None 1 8 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
174174 519 46 None -2 14 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
260 519 46 None -2 14 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
320 519 46 None -2 14 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
CHEMBL517712 519 46 None -2 14 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
DB00572 519 46 None -2 14 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
54675236 142177 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 808 15 6 12 6.3 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@](C)(OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3892218 142177 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 808 15 6 12 6.3 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@](C)(OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
53372938 128780 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 128780 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
11725334 117273 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 4 2 5 2.3 O=C(N[C@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401641 117273 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 4 2 5 2.3 O=C(N[C@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
71559319 151970 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 760 16 6 12 4.4 CN(CCNC(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3971284 151970 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 760 16 6 12 4.4 CN(CCNC(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54590927 149315 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 764 14 6 11 5.9 CN(CCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3948979 149315 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 764 14 6 11 5.9 CN(CCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54585743 62021 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 372 4 0 3 4.2 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccc(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779044 62021 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 372 4 0 3 4.2 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccc(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
57399405 68414 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 490 8 0 4 5.2 Cc1cc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cc(C)n1 10.1016/j.bmcl.2011.10.002
CHEMBL1921920 68414 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 490 8 0 4 5.2 Cc1cc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cc(C)n1 10.1016/j.bmcl.2011.10.002
24988642 68803 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 379 4 0 3 3.8 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccc(Cl)cc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924037 68803 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 379 4 0 3 3.8 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccc(Cl)cc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546737 103186 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccncc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087365 103186 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccncc1 10.1016/j.bmcl.2013.09.092
72547253 103194 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 518 6 1 4 5.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087374 103194 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 518 6 1 4 5.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2013.09.092
72547499 103238 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 519 6 1 5 4.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(C(F)(F)F)nn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087945 103238 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 519 6 1 5 4.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(C(F)(F)F)nn1 10.1016/j.bmcl.2013.09.092
72545051 103256 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 3 0 2 4.0 C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2 10.1016/j.bmcl.2013.09.092
CHEMBL3088076 103256 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 3 0 2 4.0 C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2 10.1016/j.bmcl.2013.09.092
1734 116 8 None 1 12 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm701575k
307 116 8 None 1 12 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm701575k
CHEMBL168067 116 8 None 1 12 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm701575k
11852298 13912 0 None -1 3 Human 8.6 pIC50 = 8.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL1197251 13912 0 None -1 3 Human 8.6 pIC50 = 8.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL564057 13912 0 None -1 3 Human 8.6 pIC50 = 8.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
2028 2931 77 None 1 11 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 2931 77 None 1 11 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 2931 77 None 1 11 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 2931 77 None 1 11 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 2931 77 None 1 11 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
53372938 128780 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 128780 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
2286 3134 48 None -1 29 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3134 48 None -1 29 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3134 48 None -1 29 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3134 48 None -1 29 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3134 48 None -1 29 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
14374296 101183 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 8 1 5 4.3 CCN(CC)CCCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL299142 101183 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 8 1 5 4.3 CCN(CC)CCCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
14590398 101396 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCCCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL300660 101396 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCCCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
44236338 13797 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 6 1 5 4.4 O=C(O[C@H]1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1196358 13797 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 6 1 5 4.4 O=C(O[C@H]1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL556634 13797 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 6 1 5 4.4 O=C(O[C@H]1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
14374296 101183 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 8 1 5 4.3 CCN(CC)CCCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL299142 101183 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 8 1 5 4.3 CCN(CC)CCCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
14590398 101396 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCCCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL300660 101396 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCCCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
14590402 100618 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(C)ccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL294919 100618 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(C)ccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578572 186316 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 407 6 1 5 3.1 CCN(CC)CC1CCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL48980 186316 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 407 6 1 5 3.1 CCN(CC)CC1CCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
14590403 187811 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 7 1 5 4.1 CCc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCCCC1CN(CC)CC 10.1021/jm00128a008
CHEMBL50176 187811 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 7 1 5 4.1 CCc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCCCC1CN(CC)CC 10.1021/jm00128a008
14590402 100618 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(C)ccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL294919 100618 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(C)ccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
13578572 186316 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 407 6 1 5 3.1 CCN(CC)CC1CCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL48980 186316 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 407 6 1 5 3.1 CCN(CC)CC1CCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
14590403 187811 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 7 1 5 4.1 CCc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCCCC1CN(CC)CC 10.1021/jm00048a014
CHEMBL50176 187811 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 7 1 5 4.1 CCc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCCCC1CN(CC)CC 10.1021/jm00048a014
10546275 15033 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.5 CCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL121059 15033 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.5 CCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
10499832 12029 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184134 12029 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL334093 12029 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
2726 906 64 None -18 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 906 64 None -18 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 906 64 None -18 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 906 64 None -18 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 906 64 None -18 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
3500 1498 9 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 483 7 1 5 3.9 CCCCN1C(=O)C(CC2CCCCC2)NC(=O)C21CCN(CC2)Cc1ccc2c(c1)OCCO2 10.1021/jm060051s
491774 1498 9 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 483 7 1 5 3.9 CCCCN1C(=O)C(CC2CCCCC2)NC(=O)C21CCN(CC2)Cc1ccc2c(c1)OCCO2 10.1021/jm060051s
CHEMBL1196395 1498 9 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 483 7 1 5 3.9 CCCCN1C(=O)C(CC2CCCCC2)NC(=O)C21CCN(CC2)Cc1ccc2c(c1)OCCO2 10.1021/jm060051s
1548953 205945 24 None -2 17 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 205945 24 None -2 17 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
10591874 13205 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1192001 13205 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL543177 13205 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
66592813 150284 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 9 0 3 5.6 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)c1ccccc1 nan
CHEMBL3956822 150284 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 9 0 3 5.6 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)c1ccccc1 nan
54584800 62016 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 356 5 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)Cc1cccs1 10.1016/j.bmcl.2011.03.096
CHEMBL1779039 62016 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 356 5 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)Cc1cccs1 10.1016/j.bmcl.2011.03.096
10686988 12083 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 317 8 0 3 4.2 CCCCCCOC(=O)[C@H]1CN(CC)CC[C@H]1c1ccccc1 10.1021/jm980067l
CHEMBL1184244 12083 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 317 8 0 3 4.2 CCCCCCOC(=O)[C@H]1CN(CC)CC[C@H]1c1ccccc1 10.1021/jm980067l
CHEMBL340780 12083 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 317 8 0 3 4.2 CCCCCCOC(=O)[C@H]1CN(CC)CC[C@H]1c1ccccc1 10.1021/jm980067l
10678449 22452 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 154 2 0 3 0.6 CO/N=C/[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL132698 22452 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 154 2 0 3 0.6 CO/N=C/[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
1530 2151 44 None -57 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2151 44 None -57 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2151 44 None -57 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2151 44 None -57 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2151 44 None -57 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
44236334 13898 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 nan
CHEMBL1197117 13898 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 nan
CHEMBL559931 13898 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 nan
10516408 11336 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180330 11336 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL122353 11336 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
3055 1405 43 None -1 9 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
313 1405 43 None -1 9 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
7163 1405 43 None -1 9 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
CHEMBL936 1405 43 None -1 9 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
DB01231 1405 43 None -1 9 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
10594386 11313 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180249 11313 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL118553 11313 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
72546492 103249 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 489 6 0 4 6.7 O=C(O[C@H]1C[N+]2(Cc3csc(-c4ccccc4)n3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087956 103249 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 489 6 0 4 6.7 O=C(O[C@H]1C[N+]2(Cc3csc(-c4ccccc4)n3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
52942610 19131 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 384 3 0 3 3.8 O=C(c1ccccc1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1290635 19131 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 384 3 0 3 3.8 O=C(c1ccccc1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
57402223 68809 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 413 7 0 3 4.7 CCC(CC)[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
CHEMBL1924043 68809 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 413 7 0 3 4.7 CCC(CC)[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
46890977 6654 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
CHEMBL1083723 6654 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
46891075 6735 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083926 6735 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
10757736 14339 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL120135 14339 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
10755733 11323 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.4 CCN1CCC(c2ccccc2)=C(C(=O)OCC(C)C)C1 10.1021/jm980067l
CHEMBL1180297 11323 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.4 CCN1CCC(c2ccccc2)=C(C(=O)OCC(C)C)C1 10.1021/jm980067l
CHEMBL120581 11323 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.4 CCN1CCC(c2ccccc2)=C(C(=O)OCC(C)C)C1 10.1021/jm980067l
1210 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
1213 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
2725 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
33036 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
4411 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
616 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
6976 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
716121 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
90475904 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 905 45 None -79 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
180 397 50 None -23 38 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -23 38 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -23 38 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -23 38 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -23 38 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
5648 78002 7 None -1 5 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
CHEMBL2107687 78002 7 None -1 5 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
CHEMBL2111176 78002 7 None -1 5 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
2745 3800 39 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
5572 3800 39 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
66007 3800 39 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
7315 3800 39 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
CHEMBL1490 3800 39 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
DB00376 3800 39 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
44302775 201108 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OCC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL62247 201108 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OCC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
44302776 101880 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(C)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL303758 101880 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(C)ccc2C1O3 10.1016/s0960-894x(98)00351-5
10797864 25940 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB)radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB)radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 1.0 CO/N=C(\C#N)C12CCCN(CC1)C2 10.1021/jm9702903
CHEMBL135645 25940 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB)radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB)radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 1.0 CO/N=C(\C#N)C12CCCN(CC1)C2 10.1021/jm9702903
10522202 11329 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180312 11329 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL121385 11329 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
44302900 201110 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 3 1 5 4.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OC(C)C)c34)OC21 10.1016/s0960-894x(98)00351-5
CHEMBL62251 201110 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 3 1 5 4.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OC(C)C)c34)OC21 10.1016/s0960-894x(98)00351-5
44302833 102028 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(C)c2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL304036 102028 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(C)c2C1O3 10.1016/s0960-894x(98)00351-5
10755732 12015 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184092 12015 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL332181 12015 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
1016 3690 75 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3690 75 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3690 75 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3690 75 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3690 75 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3690 75 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
10567192 11990 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1183934 11990 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL324936 11990 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
657309 59912 11 None - 0 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1CC(OC(=O)C(CO)c1ccccc1)C2 nan
CHEMBL1740585 59912 11 None - 0 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1CC(OC(=O)C(CO)c1ccccc1)C2 nan
66591963 143716 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 460 7 1 6 4.5 O=C(O[C@H]1C[N+]2(CCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3904721 143716 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 460 7 1 6 4.5 O=C(O[C@H]1C[N+]2(CCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
57400155 68344 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 448 7 0 4 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cccnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921802 68344 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 448 7 0 4 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cccnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397745 68417 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 463 8 0 5 4.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cncnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921923 68417 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 463 8 0 5 4.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cncnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397747 68424 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 481 8 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921930 68424 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 481 8 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988273 68794 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 331 4 0 3 2.8 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924028 68794 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 331 4 0 3 2.8 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCCC1 10.1016/j.bmcl.2011.10.002
57397003 68807 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 5.0 C[C@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924041 68807 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 5.0 C[C@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72543917 103243 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 522 9 2 6 2.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)NCCNC(=O)c1cnccn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087950 103243 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 522 9 2 6 2.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)NCCNC(=O)c1cnccn1 10.1016/j.bmcl.2013.09.092
72545280 103259 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 436 6 0 3 5.6 COc1cccc(C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c1 10.1016/j.bmcl.2013.09.092
CHEMBL3088079 103259 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 436 6 0 3 5.6 COc1cccc(C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c1 10.1016/j.bmcl.2013.09.092
72545284 103262 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 445 6 0 3 5.5 N#Cc1ccc(CC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cc1 10.1016/j.bmcl.2013.09.092
CHEMBL3088083 103262 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 445 6 0 3 5.5 N#Cc1ccc(CC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cc1 10.1016/j.bmcl.2013.09.092
12057539 206301 39 None 1 20 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 nan
3661 206301 39 None 1 20 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 nan
CHEMBL9751 206301 39 None 1 20 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 nan
10132599 62009 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 350 5 0 3 4.0 O=C(O[C@H]1CN2CCC1CC2)N(CCc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779032 62009 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 350 5 0 3 4.0 O=C(O[C@H]1CN2CCC1CC2)N(CCc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
71566170 144381 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 17 7 12 4.5 CC(Cc1ccc(OCC(=O)NCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3910208 144381 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 17 7 12 4.5 CC(Cc1ccc(OCC(=O)NCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
71278078 143957 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 796 15 6 12 6.2 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3cccs3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3906808 143957 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 796 15 6 12 6.2 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3cccs3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
44236340 13680 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL1195513 13680 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL554725 13680 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
52945272 19013 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 399 4 0 5 3.8 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289866 19013 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 399 4 0 5 3.8 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
13578571 100655 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)C1 10.1021/jm00128a008
CHEMBL295214 100655 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)C1 10.1021/jm00128a008
25070582 61125 21 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61125 21 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
2200 3082 38 None -22 13 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/s0960-894x(99)00528-4
328 3082 38 None -22 13 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/s0960-894x(99)00528-4
4848 3082 38 None -22 13 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/s0960-894x(99)00528-4
CHEMBL9967 3082 38 None -22 13 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/s0960-894x(99)00528-4
DB00670 3082 38 None -22 13 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/s0960-894x(99)00528-4
10726038 118927 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.6 CO/N=C(\C#N)C12CCN(CC1)C2 10.1021/jm9702903
CHEMBL344892 118927 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.6 CO/N=C(\C#N)C12CCN(CC1)C2 10.1021/jm9702903
13578571 100655 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)C1 10.1021/jm00048a014
CHEMBL295214 100655 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)C1 10.1021/jm00048a014
14590399 100808 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 393 5 2 5 2.8 CCNCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL296365 100808 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 393 5 2 5 2.8 CCNCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
24739387 187574 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 454 4 0 2 5.2 CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL498556 187574 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 454 4 0 2 5.2 CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
14590399 100808 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 393 5 2 5 2.8 CCNCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL296365 100808 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 393 5 2 5 2.8 CCNCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
44302834 201022 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 454 4 1 5 5.9 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Oc4ccccc4)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61700 201022 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 454 4 1 5 5.9 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Oc4ccccc4)ccc2C1O3 10.1016/s0960-894x(98)00351-5
127053829 144892 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 452 5 1 3 4.8 O=C(O[C@H]1C[N+]2(C/C=C/c3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
CHEMBL3914137 144892 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 452 5 1 3 4.8 O=C(O[C@H]1C[N+]2(C/C=C/c3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
69994004 153623 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 9 0 3 5.8 O=C(O[C@@H]1CC2CC[N+]1(CCCOc1ccccc1)CC2)C(c1ccccc1)c1ccccc1 nan
CHEMBL3985491 153623 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 9 0 3 5.8 O=C(O[C@@H]1CC2CC[N+]1(CCCOc1ccccc1)CC2)C(c1ccccc1)c1ccccc1 nan
87064156 159688 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 458 4 1 4 4.8 CCC1([N+]23CCC(CC2)[C@@H](OC(=O)C2(O)c4ccccc4-c4ccccc42)C3)c2ccsc21 nan
CHEMBL4109862 159688 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 458 4 1 4 4.8 CCC1([N+]23CCC(CC2)[C@@H](OC(=O)C2(O)c4ccccc4-c4ccccc42)C3)c2ccsc21 nan
52949961 19152 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 424 3 0 4 4.6 O=C(c1ccc2occc2c1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1290752 19152 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 424 3 0 4 4.6 O=C(c1ccc2occc2c1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
72546735 103184 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087363 103184 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccn1 10.1016/j.bmcl.2013.09.092
11318734 186747 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human cloned muscarinic M3 receptor expressed in CHO cells by FLIPR assayInhibition of human cloned muscarinic M3 receptor expressed in CHO cells by FLIPR assay
ChEMBL 429 6 2 5 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1021/jm800935u
CHEMBL493079 186747 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human cloned muscarinic M3 receptor expressed in CHO cells by FLIPR assayInhibition of human cloned muscarinic M3 receptor expressed in CHO cells by FLIPR assay
ChEMBL 429 6 2 5 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1021/jm800935u
4746 203183 29 None -1 4 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL1334033 203183 29 None -1 4 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL75880 203183 29 None -1 4 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
10759393 83965 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL2112589 83965 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL2219563 83965 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
4189 205195 91 None -12 34 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205195 91 None -12 34 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205195 91 None -12 34 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
52943721 19093 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 354 3 0 3 4.3 O=C(c1ccsc1)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
CHEMBL1290410 19093 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 354 3 0 3 4.3 O=C(c1ccsc1)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
46891076 6630 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 344 4 2 2 3.8 O=C(NCC1=CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083618 6630 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 344 4 2 2 3.8 O=C(NCC1=CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
10688349 12030 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184138 12030 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL334194 12030 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
176 394 63 None -1 31 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -1 31 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -1 31 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -1 31 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -1 31 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44302793 198047 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 350 2 1 4 3.9 COc1cc2c(cc1OC)C1Oc3ccc4[nH]c(C)cc4c3CN1CC2 10.1016/s0960-894x(98)00351-5
CHEMBL59347 198047 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 350 2 1 4 3.9 COc1cc2c(cc1OC)C1Oc3ccc4[nH]c(C)cc4c3CN1CC2 10.1016/s0960-894x(98)00351-5
10392705 120368 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 9 1 4 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401652 120368 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 9 1 4 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559204 120368 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 9 1 4 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
9882189 166879 26 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin)Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01192
CHEMBL4297224 166879 26 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin)Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01192
324 1894 12 None -17 9 Human 6.5 pIC50 = 6.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
6436265 1894 12 None -17 9 Human 6.5 pIC50 = 6.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
CHEMBL277642 1894 12 None -17 9 Human 6.5 pIC50 = 6.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
44302788 198938 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 2 1 5 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL59939 198938 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 2 1 5 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
2683 102415 24 None 1 16 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102415 24 None 1 16 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102415 24 None 1 16 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
5318 15400 44 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15400 44 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15400 44 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
10358345 11337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1180331 11337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL122354 11337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
71454411 78040 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 390 2 1 4 4.0 O=C1Nc2cccnc2N(C(=O)C[C@H]2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
CHEMBL2111621 78040 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 390 2 1 4 4.0 O=C1Nc2cccnc2N(C(=O)C[C@H]2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
10851853 12082 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1184242 12082 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL340561 12082 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
1209 1628 69 None -30 31 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
203 1628 69 None -30 31 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
3386 1628 69 None -30 31 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
CHEMBL41 1628 69 None -30 31 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
DB00472 1628 69 None -30 31 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
53372936 128779 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670827 128779 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
11695697 117278 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 2 1 3 3.1 O=C(N[C@H]1CN2CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
CHEMBL3401646 117278 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 2 1 3 3.1 O=C(N[C@H]1CN2CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
5310989 199193 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 3 1 5 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL60142 199193 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 3 1 5 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
10487582 28018 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL137384 28018 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
2335 11743 21 None -1 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
8478 11743 21 None -1 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL1182210 11743 21 None -1 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL221753 11743 21 None -1 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
26987 936 29 None -56 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 936 29 None -56 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 936 29 None -56 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 936 29 None -56 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 936 29 None -56 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
72545052 103257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 406 5 0 2 5.6 O=C(O[C@H]1C[N+]2(Cc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088077 103257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 406 5 0 2 5.6 O=C(O[C@H]1C[N+]2(Cc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545053 103258 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 442 5 0 2 5.8 O=C(O[C@H]1C[N+]2(Cc3ccc(F)c(F)c3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088078 103258 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 442 5 0 2 5.8 O=C(O[C@H]1C[N+]2(Cc3ccc(F)c(F)c3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
46871844 6734 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083925 6734 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
135398745 2869 108 None -27 65 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2869 108 None -27 65 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2869 108 None -27 65 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2869 108 None -27 65 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
52943921 18932 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 386 3 0 5 2.6 O=C(c1ncccn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289315 18932 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 386 3 0 5 2.6 O=C(c1ncccn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
52945165 18949 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 375 3 0 5 2.8 O=C(c1ccon1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289432 18949 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 375 3 0 5 2.8 O=C(c1ccon1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
52946068 19037 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 413 4 0 5 4.1 Cc1ccccc1CN1CCC2(CC1)CN(C(=O)c1csc(C(C)C)n1)CCO2 10.1016/j.bmcl.2010.10.016
CHEMBL1290077 19037 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 413 4 0 5 4.1 Cc1ccccc1CN1CCC2(CC1)CN(C(=O)c1csc(C(C)C)n1)CCO2 10.1016/j.bmcl.2010.10.016
46891021 6583 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 391 3 1 4 5.3 Fc1cccc(-c2cc(Cl)ccc2Cl)c1-c1nc(C2CCNCC2)no1 10.1016/j.bmcl.2010.04.127
CHEMBL1083403 6583 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 391 3 1 4 5.3 Fc1cccc(-c2cc(Cl)ccc2Cl)c1-c1nc(C2CCNCC2)no1 10.1016/j.bmcl.2010.04.127
46891488 7094 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.7 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1085507 7094 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.7 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
10785471 113217 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.9 CCCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL332320 113217 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.9 CCCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
9857572 62013 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 302 5 0 3 3.5 CCCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779036 62013 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 302 5 0 3 3.5 CCCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
3042 1386 31 None -1 15 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1386 31 None -1 15 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1386 31 None -1 15 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1386 31 None -1 15 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1386 31 None -1 15 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
11434515 259 3 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
11519741 259 3 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
4484 259 3 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
7449 259 3 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
CHEMBL1194325 259 3 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
DB08897 259 3 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
66592531 152320 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1cccs1 nan
CHEMBL3974189 152320 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1cccs1 nan
10267601 12023 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1184116 12023 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL332980 12023 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
14590395 101048 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00128a008
CHEMBL298078 101048 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00128a008
379653 101213 2 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 499 6 1 5 4.3 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Br)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL299344 101213 2 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 499 6 1 5 4.3 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Br)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578553 167556 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 4 1 6 2.5 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCOCC2)c2ccccc21 10.1021/jm00128a008
CHEMBL432886 167556 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 4 1 6 2.5 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCOCC2)c2ccccc21 10.1021/jm00128a008
14590401 187395 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Cl)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL49721 187395 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Cl)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
14590395 101048 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00048a014
CHEMBL298078 101048 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00048a014
379653 101213 2 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 499 6 1 5 4.3 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Br)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL299344 101213 2 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 499 6 1 5 4.3 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Br)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
13578553 167556 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 4 1 6 2.5 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCOCC2)c2ccccc21 10.1021/jm00048a014
CHEMBL432886 167556 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 4 1 6 2.5 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCOCC2)c2ccccc21 10.1021/jm00048a014
14590401 187395 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Cl)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL49721 187395 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Cl)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
10663572 13048 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1190784 13048 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL541584 13048 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
10614695 12051 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184188 12051 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL338280 12051 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
2284 3133 27 None -10 28 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3133 27 None -10 28 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3133 27 None -10 28 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3133 27 None -10 28 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3133 27 None -10 28 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
11057 175575 19 None -2 20 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 175575 19 None -2 20 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 175575 19 None -2 20 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 175575 19 None -2 20 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
124087 1362 106 None -9 15 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1362 106 None -9 15 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1362 106 None -9 15 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1362 106 None -9 15 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1362 106 None -9 15 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
10660 14298 55 None -2 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 14298 55 None -2 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
11793999 12009 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184074 12009 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL331516 12009 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
25014630 83126 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
CHEMBL2203713 83126 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
10852843 11819 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1182713 11819 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL262303 11819 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
5353853 17803 41 None -13 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17803 41 None -13 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17803 41 None -13 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
135466875 188526 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 769 25 5 10 6.6 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
CHEMBL510340 188526 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 769 25 5 10 6.6 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
10567372 12025 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12025 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12025 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12025 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
277 1274 55 None -11 45 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1274 55 None -11 45 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1274 55 None -11 45 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1274 55 None -11 45 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1274 55 None -11 45 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
657255 197406 29 None -11 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 197406 29 None -11 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
3013847 188328 1 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 741 23 5 10 5.8 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
CHEMBL507760 188328 1 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 741 23 5 10 5.8 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
1212 1632 45 None -407 65 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1632 45 None -407 65 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1632 45 None -407 65 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1632 45 None -407 65 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1632 45 None -407 65 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
4011 81996 43 None -14 23 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81996 43 None -14 23 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
66592626 151269 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 474 8 1 6 4.9 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3965159 151269 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 474 8 1 6 4.9 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
52942402 19023 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4cccc(Cl)c4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289983 19023 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4cccc(Cl)c4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
57392514 68428 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 464 8 0 5 4.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccncc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921934 68428 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 464 8 0 5 4.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccncc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57400423 68804 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 4 2.6 CN1CCC(OC(=O)C(C)(c2ccccc2)N2CCCC2)CC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924038 68804 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 4 2.6 CN1CCC(OC(=O)C(C)(c2ccccc2)N2CCCC2)CC1 10.1016/j.bmcl.2011.10.002
57393501 68805 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 328 4 0 4 2.6 CC(C(=O)O[C@H]1CN2CCC1CC2)(c1ccccc1)N1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924039 68805 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 328 4 0 4 2.6 CC(C(=O)O[C@H]1CN2CCC1CC2)(c1ccccc1)N1CCCC1 10.1016/j.bmcl.2011.10.002
57403965 68810 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 399 7 0 3 4.3 CCCC[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
CHEMBL1924044 68810 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 399 7 0 3 4.3 CCCC[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
1734 116 8 None 1 12 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
307 116 8 None 1 12 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL168067 116 8 None 1 12 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
44233401 13513 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 nan
CHEMBL1194321 13513 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 nan
CHEMBL551327 13513 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 nan
66592194 150055 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 502 9 1 6 4.8 O=C(O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3955111 150055 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 502 9 1 6 4.8 O=C(O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
10133281 62017 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 5 0 5 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccs1)Cc1cccs1 10.1016/j.bmcl.2011.03.096
CHEMBL1779040 62017 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 5 0 5 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccs1)Cc1cccs1 10.1016/j.bmcl.2011.03.096
122238756 146495 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 734 14 5 10 6.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c(NC=O)c3)ccc21)[C@H]1CC[C@H](c2cccc3c2C(C)(C(=O)O)c2ccccc2O3)CC1 nan
CHEMBL3926721 146495 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 734 14 5 10 6.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c(NC=O)c3)ccc21)[C@H]1CC[C@H](c2cccc3c2C(C)(C(=O)O)c2ccccc2O3)CC1 nan
52943879 19153 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 388 3 0 4 3.7 Cc1ccc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)o1 10.1016/j.bmcl.2010.10.016
CHEMBL1290753 19153 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 388 3 0 4 3.7 Cc1ccc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)o1 10.1016/j.bmcl.2010.10.016
46891179 6340 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1082365 6340 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
10573693 11325 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.5 CCN1CCC(c2ccccc2)=C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
CHEMBL1180305 11325 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.5 CCN1CCC(c2ccccc2)=C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
CHEMBL120963 11325 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.5 CCN1CCC(c2ccccc2)=C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
10567372 12025 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12025 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12025 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12025 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10595006 11340 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
CHEMBL1180343 11340 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
CHEMBL123099 11340 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
10595006 11340 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL1180343 11340 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL123099 11340 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
10521205 11324 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180298 11324 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL120599 11324 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
10684720 11988 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1183926 11988 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL324712 11988 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
44356367 117988 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 266 3 0 2 2.2 C[N+](C)(C)CC#CCOC(=O)c1cccc(Cl)c1 10.1021/jm9702903
CHEMBL341447 117988 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 266 3 0 2 2.2 C[N+](C)(C)CC#CCOC(=O)c1cccc(Cl)c1 10.1021/jm9702903
44302813 101460 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 362 2 1 4 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL301041 101460 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 362 2 1 4 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
10610375 11317 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL1180284 11317 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL120109 11317 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
10610375 11317 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm301774u
CHEMBL1180284 11317 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm301774u
CHEMBL120109 11317 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm301774u
49853884 90252 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 265 3 1 3 1.2 O=C(CN1CCN2CCC[C@H]2C1)NC1CCCCC1 10.1016/j.bmc.2013.02.058
CHEMBL2391353 90252 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 265 3 1 3 1.2 O=C(CN1CCN2CCC[C@H]2C1)NC1CCCCC1 10.1016/j.bmc.2013.02.058
2230 461 55 None -588 10 Human 4.2 pIC50 = 4.2 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
296 461 55 None -588 10 Human 4.2 pIC50 = 4.2 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
CHEMBL7303 461 55 None -588 10 Human 4.2 pIC50 = 4.2 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
DB04365 461 55 None -588 10 Human 4.2 pIC50 = 4.2 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
3013845 188163 1 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 729 21 5 11 5.1 CCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL505197 188163 1 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 729 21 5 11 5.1 CCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
10460514 120370 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401658 120370 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559206 120370 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
9798900 62806 0 None - 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmcl.2011.03.096
CHEMBL1779047 62806 0 None - 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmcl.2011.03.096
CHEMBL1789446 62806 0 None - 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmcl.2011.03.096
11569908 13888 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL1197028 13888 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL559106 13888 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
57397742 68408 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 487 7 0 4 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cc4ccccc4o3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921912 68408 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 487 7 0 4 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cc4ccccc4o3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72543918 103244 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 535 10 2 5 3.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)NCCCNC(=O)c1ccccn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087951 103244 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 535 10 2 5 3.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)NCCCNC(=O)c1ccccn1 10.1016/j.bmcl.2013.09.092
66592271 149422 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 448 8 1 5 3.7 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
CHEMBL3949833 149422 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 448 8 1 5 3.7 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
66592394 152871 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 462 9 1 5 4.1 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
CHEMBL3978891 152871 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 462 9 1 5 4.1 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
44236101 13914 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
CHEMBL1197261 13914 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
CHEMBL564515 13914 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
306 3400 18 None -4 5 Human 7.2 pIC50 = 7.2 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
3536 3400 18 None -4 5 Human 7.2 pIC50 = 7.2 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
53930639 3400 18 None -4 5 Human 7.2 pIC50 = 7.2 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
9577995 3400 18 None -4 5 Human 7.2 pIC50 = 7.2 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
CHEMBL134641 3400 18 None -4 5 Human 7.2 pIC50 = 7.2 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
67548544 120369 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 559 8 0 3 7.1 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCOc3ccc(-c4ccccc4)cc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
CHEMBL3401656 120369 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 559 8 0 3 7.1 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCOc3ccc(-c4ccccc4)cc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
CHEMBL3559205 120369 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 559 8 0 3 7.1 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCOc3ccc(-c4ccccc4)cc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
2200 3082 38 None -22 13 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00128a008
328 3082 38 None -22 13 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00128a008
4848 3082 38 None -22 13 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00128a008
CHEMBL9967 3082 38 None -22 13 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00128a008
DB00670 3082 38 None -22 13 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00128a008
13578549 100804 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCN(CC)CC1CCCCN1CCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL296317 100804 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCN(CC)CC1CCCCN1CCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578549 100804 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCN(CC)CC1CCCCN1CCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL296317 100804 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCN(CC)CC1CCCCN1CCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
107867 2927 48 None -12 10 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
309 2927 48 None -12 10 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
CHEMBL17045 2927 48 None -12 10 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
14590400 176888 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 8 1 5 4.3 CCCN(CCC)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL46390 176888 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 8 1 5 4.3 CCCN(CCC)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
107867 2927 48 None -12 10 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
309 2927 48 None -12 10 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
CHEMBL17045 2927 48 None -12 10 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
14590400 176888 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 8 1 5 4.3 CCCN(CCC)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL46390 176888 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 8 1 5 4.3 CCCN(CCC)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL1200633 206858 3 None -4 8 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(CC[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(CC[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
13583409 11350 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %
ChEMBL 128 3 1 1 -0.0 OCC[N+]1(C2CC2)CC1 10.1021/jm00153a012
CHEMBL1180358 11350 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %
ChEMBL 128 3 1 1 -0.0 OCC[N+]1(C2CC2)CC1 10.1021/jm00153a012
CHEMBL123573 11350 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %
ChEMBL 128 3 1 1 -0.0 OCC[N+]1(C2CC2)CC1 10.1021/jm00153a012
135423423 188419 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 813 27 5 11 7.5 CCCCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL508807 188419 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 813 27 5 11 7.5 CCCCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
52942628 18896 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 374 3 0 4 3.4 O=C(c1ccco1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289081 18896 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 374 3 0 4 3.4 O=C(c1ccco1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
52946249 18897 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 390 3 0 4 3.9 O=C(c1cccs1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289082 18897 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 390 3 0 4 3.9 O=C(c1cccs1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
3013846 187656 2 None 1 5 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL499519 187656 2 None 1 5 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
10567372 12025 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12025 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12025 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12025 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
67547950 120364 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 456 6 0 3 4.9 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCn3cccc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
CHEMBL3401655 120364 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 456 6 0 3 4.9 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCn3cccc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
CHEMBL3559199 120364 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 456 6 0 3 4.9 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCn3cccc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
107782 14330 16 None -1 5 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
67151996 14330 16 None -1 5 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
CHEMBL1201207 14330 16 None -1 5 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
1224 1404 79 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1404 79 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1404 79 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1404 79 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1404 79 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1404 79 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3191 102385 93 None -6 25 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102385 93 None -6 25 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
54586723 62015 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 288 3 0 3 3.1 CC(C)N(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779038 62015 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 288 3 0 3 3.1 CC(C)N(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
1836 2554 56 None -42 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 2554 56 None -42 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 2554 56 None -42 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 2554 56 None -42 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 2554 56 None -42 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
10782321 12018 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
CHEMBL1184098 12018 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
CHEMBL332405 12018 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
10854879 11312 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180239 11312 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL118241 11312 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10636001 11320 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1180290 11320 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL120329 11320 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
10777692 11322 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180296 11322 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL120539 11322 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
3158 55974 21 None -104 20 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55974 21 None -104 20 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
44233175 13905 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
CHEMBL1197209 13905 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
CHEMBL562655 13905 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
50925543 18984 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4Cl)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289654 18984 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4Cl)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
57393502 68811 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 410 7 0 4 3.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCCC#N)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924045 68811 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 410 7 0 4 3.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCCC#N)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
76309856 103171 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 457 6 1 6 3.9 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1nncs1 10.1016/j.bmcl.2013.09.092
CHEMBL3087243 103171 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 457 6 1 6 3.9 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1nncs1 10.1016/j.bmcl.2013.09.092
10096508 176449 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 475 5 1 5 4.8 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCCC1 10.1021/jm00128a008
CHEMBL46315 176449 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 475 5 1 5 4.8 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCCC1 10.1021/jm00128a008
10096508 176449 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 475 5 1 5 4.8 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCCC1 10.1021/jm00048a014
CHEMBL46315 176449 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 475 5 1 5 4.8 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCCC1 10.1021/jm00048a014
54583839 62012 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 288 4 0 3 3.1 CCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779035 62012 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 288 4 0 3 3.1 CCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
118728611 117276 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 294 4 2 4 1.6 CCC(O)(C(=O)N[C@H]1CN2CCC1CC2)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401644 117276 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 294 4 2 4 1.6 CCC(O)(C(=O)N[C@H]1CN2CCC1CC2)c1cccs1 10.1016/j.bmcl.2015.02.065
9903030 62019 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 350 4 0 3 4.2 Cc1ccc(N(Cc2ccccc2)C(=O)O[C@H]2CN3CCC2CC3)cc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779042 62019 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 350 4 0 3 4.2 Cc1ccc(N(Cc2ccccc2)C(=O)O[C@H]2CN3CCC2CC3)cc1 10.1016/j.bmcl.2011.03.096
6726 1254 46 None -6 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1254 46 None -6 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1254 46 None -6 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1254 46 None -6 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1254 46 None -6 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
10784004 13276 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1192621 13276 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL543890 13276 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
5282593 54972 25 None -1 5 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
CHEMBL1319362 54972 25 None -1 5 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
CHEMBL1618018 54972 25 None -1 5 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
44333822 4597 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 406 2 1 4 4.8 O=C1Nc2cccnc2N(C(=S)CC2CCCN3CCCC[C@@H]23)c2ccccc21 10.1016/s0960-894x(99)00528-4
CHEMBL103189 4597 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 406 2 1 4 4.8 O=C1Nc2cccnc2N(C(=S)CC2CCCN3CCCC[C@@H]23)c2ccccc21 10.1016/s0960-894x(99)00528-4
10048670 106972 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 436 4 1 5 4.3 O=C1Nc2cccnc2N(C(=O)CSCC2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
CHEMBL318316 106972 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 436 4 1 5 4.3 O=C1Nc2cccnc2N(C(=O)CSCC2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
1547484 927 70 None -5 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 927 70 None -5 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 927 70 None -5 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 927 70 None -5 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 927 70 None -5 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
135398737 944 89 None -10 91 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 944 89 None -10 91 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 944 89 None -10 91 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 944 89 None -10 91 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 944 89 None -10 91 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
52949883 19130 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 5 0 3 4.6 CCOc1ccccc1C(=O)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
CHEMBL1290634 19130 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 5 0 3 4.6 CCOc1ccccc1C(=O)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
54585742 62008 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779031 62008 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
66592485 150694 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 500 9 2 7 4.4 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3O)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3960065 150694 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 500 9 2 7 4.4 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3O)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
54673528 152224 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 790 15 6 11 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3ccccc3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3973386 152224 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 790 15 6 11 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3ccccc3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
127053833 147267 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 7 0 4 5.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL3932738 147267 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 7 0 4 5.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
44333541 4684 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 419 4 2 5 3.2 O=C1Nc2cccnc2N(C(=O)CNCC2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
CHEMBL103785 4684 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 419 4 2 5 3.2 O=C1Nc2cccnc2N(C(=O)CNCC2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
100826 90253 65 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 185 3 2 3 -0.6 CC(C)NC(=O)CN1CCNCC1 10.1016/j.bmc.2013.02.058
CHEMBL2391356 90253 65 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 185 3 2 3 -0.6 CC(C)NC(=O)CN1CCNCC1 10.1016/j.bmc.2013.02.058
2247 502 77 None -19 41 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -19 41 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -19 41 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -19 41 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -19 41 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
10827157 11332 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.2 CCN1CC=C(c2ccccc2)C(C(=O)OCC(C)C)C1 10.1021/jm980067l
CHEMBL1180317 11332 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.2 CCN1CC=C(c2ccccc2)C(C(=O)OCC(C)C)C1 10.1021/jm980067l
CHEMBL121552 11332 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.2 CCN1CC=C(c2ccccc2)C(C(=O)OCC(C)C)C1 10.1021/jm980067l
10854880 11316 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1180282 11316 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL120080 11316 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
68835 71949 49 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 225 3 2 3 0.3 O=C(CN1CCNCC1)NC1CCCCC1 10.1016/j.bmc.2013.02.058
CHEMBL1983100 71949 49 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 225 3 2 3 0.3 O=C(CN1CCNCC1)NC1CCCCC1 10.1016/j.bmc.2013.02.058
10549581 11344 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.4 CCN1CC=C(c2ccccc2)C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
CHEMBL1180349 11344 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.4 CCN1CC=C(c2ccccc2)C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
CHEMBL123198 11344 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.4 CCN1CC=C(c2ccccc2)C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
10760249 11318 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm301774u
CHEMBL1180285 11318 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm301774u
CHEMBL120119 11318 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm301774u
10760249 11318 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
CHEMBL1180285 11318 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
CHEMBL120119 11318 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
2551 782 23 None -346 11 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
298 782 23 None -346 11 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
488 782 23 None -346 11 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
CHEMBL965 782 23 None -346 11 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
DB00411 782 23 None -346 11 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
10538337 12005 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL1184062 12005 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL330885 12005 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1 10.1021/jm980067l
118728611 117276 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 294 4 2 4 1.6 CCC(O)(C(=O)N[C@H]1CN2CCC1CC2)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401644 117276 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 294 4 2 4 1.6 CCC(O)(C(=O)N[C@H]1CN2CCC1CC2)c1cccs1 10.1016/j.bmcl.2015.02.065
66592447 147170 0 None - 0 Human 8.0 pIC50 = 8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.4 O=C(O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3931995 147170 0 None - 0 Human 8.0 pIC50 = 8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.4 O=C(O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
100 3745 52 None -8 55 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3745 52 None -8 55 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3745 52 None -8 55 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3745 52 None -8 55 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3745 52 None -8 55 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2551 782 23 None -346 11 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
298 782 23 None -346 11 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
488 782 23 None -346 11 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
CHEMBL965 782 23 None -346 11 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
DB00411 782 23 None -346 11 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
10638050 11310 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL116601 11310 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180202 11310 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
44235638 193644 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 347 2 0 3 3.6 O=C(O[C@H]1CN2CCC1CC2)C1c2ccccc2CCc2ccccc21 10.1021/jm900132z
CHEMBL551525 193644 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 347 2 0 3 3.6 O=C(O[C@H]1CN2CCC1CC2)C1c2ccccc2CCc2ccccc21 10.1021/jm900132z
11498 2970 33 None -38 5 Human 6.0 pIC50 = 6.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/s0960-894x(98)00351-5
4995951 2970 33 None -38 5 Human 6.0 pIC50 = 6.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/s0960-894x(98)00351-5
CHEMBL59898 2970 33 None -38 5 Human 6.0 pIC50 = 6.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/s0960-894x(98)00351-5
2200 3082 38 None -15 13 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
328 3082 38 None -15 13 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
4848 3082 38 None -15 13 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
CHEMBL9967 3082 38 None -15 13 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
DB00670 3082 38 None -15 13 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
10846833 49536 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 225 0 0 5 1.7 CN1CCC2=C(C1)c1nsnc1SC2 10.1021/jm9705216
CHEMBL15675 49536 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 225 0 0 5 1.7 CN1CCC2=C(C1)c1nsnc1SC2 10.1021/jm9705216
10547222 114288 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333940 114288 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
2812 4711 96 None -22 34 Human 5.0 pIC50 = 5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4711 96 None -22 34 Human 5.0 pIC50 = 5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
164612037 184795 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 184795 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 192366 0 None -8 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192366 0 None -8 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192366 0 None -8 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 192417 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192417 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192417 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 192429 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192429 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192429 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
4120 5857 6 None 1 3 Rat 9.4 pKd = 9.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 318 4 1 4 1.1 C[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL107979 5857 6 None 1 3 Rat 9.4 pKd = 9.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 318 4 1 4 1.1 C[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL293927 5857 6 None 1 3 Rat 9.4 pKd = 9.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 318 4 1 4 1.1 C[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
174174 519 46 None -1 14 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00170a010
260 519 46 None -1 14 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00170a010
320 519 46 None -1 14 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00170a010
CHEMBL517712 519 46 None -1 14 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00170a010
DB00572 519 46 None -1 14 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00170a010
11968014 12649 4 None -1 9 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/jm00170a010
CHEMBL1187846 12649 4 None -1 9 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/jm00170a010
14753629 13557 0 None -1 3 Rat 8.9 pKd = 8.9 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 302 5 2 4 1.9 N=CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL1194660 13557 0 None -1 3 Rat 8.9 pKd = 8.9 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 302 5 2 4 1.9 N=CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL553066 13557 0 None -1 3 Rat 8.9 pKd = 8.9 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 302 5 2 4 1.9 N=CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
9913341 81746 3 None -25 5 Human 6.8 pKd = 6.8 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 81746 3 None -25 5 Human 6.8 pKd = 6.8 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL553058 81746 3 None -25 5 Human 6.8 pKd = 6.8 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
44418764 81747 0 None -8 5 Human 6.8 pKd = 6.8 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 81747 0 None -8 5 Human 6.8 pKd = 6.8 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
14753624 13624 0 None 2 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 317 4 3 4 1.2 N=C(N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL1195123 13624 0 None 2 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 317 4 3 4 1.2 N=C(N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL553894 13624 0 None 2 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 317 4 3 4 1.2 N=C(N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
5861 11180 10 None -1 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 304 4 1 3 2.1 C[N+]1(C)C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL1179176 11180 10 None -1 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 304 4 1 3 2.1 C[N+]1(C)C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL63452 11180 10 None -1 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 304 4 1 3 2.1 C[N+]1(C)C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
3636 11043 5 None -1 3 Rat 6.7 pKd = 6.7 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL1178342 11043 5 None -1 3 Rat 6.7 pKd = 6.7 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL21823 11043 5 None -1 3 Rat 6.7 pKd = 6.7 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
14753634 13615 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 4 2 4 2.3 CC(=N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL1195059 13615 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 4 2 4 2.3 CC(=N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL553783 13615 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 4 2 4 2.3 CC(=N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
14753637 13378 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 330 4 2 5 1.3 CC(=N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL1193366 13378 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 330 4 2 5 1.3 CC(=N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL544759 13378 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 330 4 2 5 1.3 CC(=N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
14753627 13594 0 None 1 3 Rat 8.4 pKd = 8.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 331 4 3 5 0.2 N=C(N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL1194941 13594 0 None 1 3 Rat 8.4 pKd = 8.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 331 4 3 5 0.2 N=C(N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL553562 13594 0 None 1 3 Rat 8.4 pKd = 8.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 331 4 3 5 0.2 N=C(N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
14753632 13397 0 None -1 3 Rat 8.3 pKd = 8.3 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 5 2 5 0.9 N=CN1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL1193564 13397 0 None -1 3 Rat 8.3 pKd = 8.3 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 5 2 5 0.9 N=CN1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL544993 13397 0 None -1 3 Rat 8.3 pKd = 8.3 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 5 2 5 0.9 N=CN1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
16094788 141383 0 None -125 5 Human 7.2 pKd = 7.2 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL386983 141383 0 None -125 5 Human 7.2 pKd = 7.2 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
367 3764 8 None 2 8 Human 11.0 pKi = 11.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
5487427 3764 8 None 2 8 Human 11.0 pKi = 11.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
8592 3764 8 None 2 8 Human 11.0 pKi = 11.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL1900528 3764 8 None 2 8 Human 11.0 pKi = 11.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL3305968 3764 8 None 2 8 Human 11.0 pKi = 11.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL4650755 3764 8 None 2 8 Human 11.0 pKi = 11.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
DB01409 3764 8 None 2 8 Human 11.0 pKi = 11.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
367 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
9874175 58230 1 None 34 2 Human 11.0 pKi = 11 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683934 58230 1 None 34 2 Human 11.0 pKi = 11 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
367 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3764 8 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
59291417 112325 0 None -1 3 Rat 10.7 pKi = 10.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 343 3 1 3 4.3 C[N+]12CCC(OC(=O)Nc3ccsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298595 112325 0 None -1 3 Rat 10.7 pKi = 10.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 343 3 1 3 4.3 C[N+]12CCC(OC(=O)Nc3ccsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307168 112325 0 None -1 3 Rat 10.7 pKi = 10.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 343 3 1 3 4.3 C[N+]12CCC(OC(=O)Nc3ccsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
367 3764 8 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3764 8 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3764 8 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3764 8 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3764 8 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3764 8 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3764 8 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
11504490 192003 0 None 39 3 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL521523 192003 0 None 39 3 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
367 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
5487427 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
8592 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
CHEMBL1900528 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
CHEMBL3305968 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
CHEMBL4650755 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
DB01409 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
367 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
5487427 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
8592 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
CHEMBL1900528 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
CHEMBL3305968 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
CHEMBL4650755 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
DB01409 3764 8 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
25005841 112322 0 None -1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.4 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298599 112322 0 None -1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.4 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307130 112322 0 None -1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.4 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
10109130 132494 0 None 6 2 Human 10.3 pKi = 10.3 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 359 3 1 5 3.2 CO[C@]1(C#CC(O)(c2cccs2)c2cccs2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL370232 132494 0 None 6 2 Human 10.3 pKi = 10.3 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 359 3 1 5 3.2 CO[C@]1(C#CC(O)(c2cccs2)c2cccs2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
72712272 105974 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 390 4 0 5 3.4 CC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
CHEMBL3091665 105974 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 390 4 0 5 3.4 CC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
CHEMBL3139995 105974 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 390 4 0 5 3.4 CC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
11857427 118547 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426693 118547 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
59291402 112289 0 None 1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1ccsc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298588 112289 0 None 1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1ccsc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305766 112289 0 None 1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1ccsc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
25195533 77983 1 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2103803 77983 1 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2110584 77983 1 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11519069 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11519070 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
4816 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
7354 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
CHEMBL1187833 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
DB09076 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
72712270 105973 0 None - 1 Human 10.2 pKi = 10.2 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 380 4 1 4 2.2 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)(c3ccccc3)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3091664 105973 0 None - 1 Human 10.2 pKi = 10.2 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 380 4 1 4 2.2 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)(c3ccccc3)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3139994 105973 0 None - 1 Human 10.2 pKi = 10.2 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 380 4 1 4 2.2 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)(c3ccccc3)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL5074599 212548 0 None 2 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
12165 898 4 None -15 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 10.1021/acs.jmedchem.2c00609
90200922 898 4 None -15 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 10.1021/acs.jmedchem.2c00609
CHEMBL5172865 898 4 None -15 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 10.1021/acs.jmedchem.2c00609
90213810 190669 0 None -2 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 750 16 5 11 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5190387 190669 0 None -2 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 750 16 5 11 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
25195533 77983 1 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2103803 77983 1 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2110584 77983 1 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
59291241 112317 0 None -1 3 Rat 10.2 pKi = 10.2 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.7 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298596 112317 0 None -1 3 Rat 10.2 pKi = 10.2 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.7 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307116 112317 0 None -1 3 Rat 10.2 pKi = 10.2 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.7 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
156011965 176718 0 None 3 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 176718 0 None 3 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
11434515 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
11519741 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
4484 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
7449 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
CHEMBL1194325 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
DB08897 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
10143956 13798 0 None -1 3 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL1196359 13798 0 None -1 3 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL556635 13798 0 None -1 3 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
156009673 177679 0 None 1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4633816 177679 0 None 1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650683 177679 0 None 1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156014812 177687 0 None 1 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4647437 177687 0 None 1 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650736 177687 0 None 1 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
367 3764 8 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
5487427 3764 8 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
8592 3764 8 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL1900528 3764 8 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL3305968 3764 8 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL4650755 3764 8 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
DB01409 3764 8 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
168287036 190910 0 None -3 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5193853 190910 0 None -3 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
10372344 118541 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 675 12 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
CHEMBL3426687 118541 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 675 12 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
10291977 72553 0 None 5 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 359 3 1 5 3.2 CO[C@]1(C#CC(O)(c2ccsc2)c2ccsc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200401 72553 0 None 5 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 359 3 1 5 3.2 CO[C@]1(C#CC(O)(c2ccsc2)c2ccsc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
11852298 13912 0 None -1 3 Human 10.1 pKi = 10.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1197251 13912 0 None -1 3 Human 10.1 pKi = 10.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL564057 13912 0 None -1 3 Human 10.1 pKi = 10.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
156015300 177018 0 None 4 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177018 0 None 4 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
54580128 61465 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 723 20 6 7 7.2 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(CO)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773196 61465 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 723 20 6 7 7.2 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(CO)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
15599352 108136 0 None -2 2 Rat 10.0 pKi = 10.0 Binding
The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL320611 108136 0 None -2 2 Rat 10.0 pKi = 10.0 Binding
The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL5070876 212475 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076637 212683 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)cc1OC 10.1021/acs.jmedchem.1c00204
164620727 185504 0 None -7 2 Human 10.0 pKi = 10 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 821 16 6 9 6.8 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)NCCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4871517 185504 0 None -7 2 Human 10.0 pKi = 10 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 821 16 6 9 6.8 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)NCCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
59291493 112324 0 None -1 3 Rat 10.0 pKi = 10 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 362 3 1 4 3.9 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccc(F)cc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298600 112324 0 None -1 3 Rat 10.0 pKi = 10 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 362 3 1 4 3.9 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccc(F)cc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307158 112324 0 None -1 3 Rat 10.0 pKi = 10 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 362 3 1 4 3.9 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccc(F)cc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
10461973 118551 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 655 15 6 8 4.9 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)NCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426697 118551 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 655 15 6 8 4.9 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)NCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
87142783 118558 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3426704 118558 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548101 123880 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3639442 123880 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548063 124681 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645274 124681 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548134 124682 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645275 124682 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057795 124683 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645276 124683 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791483 124684 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645277 124684 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548074 124685 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645278 124685 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548089 124686 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645279 124686 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548094 124687 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645280 124687 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548099 124688 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645281 124688 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
68057677 124689 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645282 124689 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548122 124690 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645283 124690 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548079 124691 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645284 124691 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548056 124692 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645285 124692 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548067 124693 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645286 124693 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548141 124694 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645287 124694 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548102 124695 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645288 124695 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057804 124696 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645289 124696 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548054 124697 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645290 124697 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548125 124698 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645291 124698 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548107 124700 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645293 124700 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548081 124702 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645295 124702 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548093 124705 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645298 124705 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548138 124713 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645305 124713 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548130 124716 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645308 124716 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548100 124717 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645309 124717 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791606 124719 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645311 124719 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843742 124722 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645314 124722 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548073 124733 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645324 124733 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548112 124734 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645325 124734 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548061 124735 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645326 124735 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548066 124736 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645327 124736 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548076 124737 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645328 124737 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548117 124739 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645330 124739 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548121 124741 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645332 124741 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548110 124742 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645333 124742 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548135 124744 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645335 124744 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548142 124751 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645341 124751 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548083 124753 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645343 124753 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548140 124755 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645345 124755 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548050 124756 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645346 124756 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548069 124758 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645348 124758 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548115 124760 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645350 124760 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548103 124761 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645351 124761 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548057 124762 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645352 124762 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548090 124766 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
CHEMBL3645356 124766 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
59548133 124768 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645358 124768 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548068 124769 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645359 124769 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548105 124771 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 124771 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548071 124772 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645362 124772 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
56953428 124773 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645363 124773 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
49785227 124775 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645365 124775 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
49785225 127945 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3666068 127945 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
49785142 142740 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 C[C@@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3896828 142740 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 C[C@@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
118405970 151273 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 848 17 5 8 7.6 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NCCc1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3965175 151273 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 848 17 5 8 7.6 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NCCc1ccc(O)c2[nH]c(=O)ccc12 nan
118405964 160232 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.3 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1 nan
CHEMBL4114219 160232 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.3 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1 nan
59548101 123880 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3639442 123880 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548063 124681 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645274 124681 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548134 124682 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645275 124682 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057795 124683 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645276 124683 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791483 124684 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645277 124684 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548074 124685 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645278 124685 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548089 124686 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645279 124686 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548094 124687 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645280 124687 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548099 124688 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645281 124688 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
68057677 124689 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645282 124689 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548122 124690 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645283 124690 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548079 124691 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645284 124691 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548056 124692 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645285 124692 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548067 124693 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645286 124693 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548141 124694 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645287 124694 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548102 124695 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645288 124695 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057804 124696 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645289 124696 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548054 124697 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645290 124697 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548125 124698 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645291 124698 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548107 124700 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645293 124700 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548081 124702 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645295 124702 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548093 124705 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645298 124705 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548138 124713 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645305 124713 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548130 124716 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645308 124716 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548100 124717 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645309 124717 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791606 124719 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645311 124719 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843742 124722 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645314 124722 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843735 124726 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.4 CC(Cc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645318 124726 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.4 CC(Cc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548065 124731 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645322 124731 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548073 124733 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645324 124733 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548112 124734 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645325 124734 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548061 124735 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645326 124735 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548066 124736 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645327 124736 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548076 124737 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645328 124737 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548117 124739 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645330 124739 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548058 124740 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 124740 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548121 124741 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645332 124741 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548110 124742 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645333 124742 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548135 124744 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645335 124744 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548142 124751 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645341 124751 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548083 124753 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645343 124753 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548140 124755 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645345 124755 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548050 124756 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645346 124756 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548069 124758 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645348 124758 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548103 124761 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645351 124761 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548057 124762 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645352 124762 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548090 124766 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
CHEMBL3645356 124766 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
59548133 124768 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645358 124768 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548068 124769 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645359 124769 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
91667374 124770 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.4 C[C@@H](Cc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645360 124770 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.4 C[C@@H](Cc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548105 124771 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 124771 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548071 124772 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645362 124772 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
56953428 124773 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645363 124773 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548055 124774 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 808 14 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645364 124774 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 808 14 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
49785227 124775 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645365 124775 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548101 123880 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3639442 123880 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548063 124681 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645274 124681 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548134 124682 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645275 124682 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057795 124683 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645276 124683 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791483 124684 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645277 124684 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548074 124685 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645278 124685 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548089 124686 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645279 124686 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548094 124687 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645280 124687 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548099 124688 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645281 124688 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
68057677 124689 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645282 124689 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548079 124691 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645284 124691 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548056 124692 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645285 124692 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548067 124693 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645286 124693 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548141 124694 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645287 124694 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548102 124695 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645288 124695 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057804 124696 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645289 124696 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548054 124697 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645290 124697 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548125 124698 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645291 124698 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548107 124700 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645293 124700 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548081 124702 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645295 124702 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548093 124705 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645298 124705 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
49785226 124708 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645300 124708 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548138 124713 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645305 124713 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548130 124716 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645308 124716 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548100 124717 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645309 124717 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791606 124719 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645311 124719 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843742 124722 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645314 124722 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843735 124726 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.4 CC(Cc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645318 124726 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.4 CC(Cc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548065 124731 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645322 124731 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548073 124733 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645324 124733 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548112 124734 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645325 124734 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548061 124735 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645326 124735 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548066 124736 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645327 124736 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548076 124737 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645328 124737 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548117 124739 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645330 124739 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548058 124740 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 124740 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548121 124741 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645332 124741 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548110 124742 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645333 124742 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548135 124744 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645335 124744 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548142 124751 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645341 124751 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548083 124753 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645343 124753 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548140 124755 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645345 124755 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548050 124756 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645346 124756 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548069 124758 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645348 124758 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548103 124761 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645351 124761 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548057 124762 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645352 124762 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548090 124766 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
CHEMBL3645356 124766 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
59548133 124768 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645358 124768 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548068 124769 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645359 124769 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548071 124772 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645362 124772 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
56953428 124773 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645363 124773 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548055 124774 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 808 14 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645364 124774 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 808 14 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
49785227 124775 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645365 124775 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
90654070 127943 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1cccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3666066 127943 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1cccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
90654071 127944 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 17 6 9 5.9 C[C@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3666067 127944 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 17 6 9 5.9 C[C@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
49785225 127945 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3666068 127945 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
16065402 67585 0 None -1 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 428 9 1 3 4.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910848 67585 0 None -1 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 428 9 1 3 4.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2)C1 10.1021/jm200884j
174174 519 46 None -1 14 Rat 9.9 pKi = 9.9 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00059a009
260 519 46 None -1 14 Rat 9.9 pKi = 9.9 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00059a009
320 519 46 None -1 14 Rat 9.9 pKi = 9.9 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00059a009
CHEMBL517712 519 46 None -1 14 Rat 9.9 pKi = 9.9 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00059a009
DB00572 519 46 None -1 14 Rat 9.9 pKi = 9.9 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00059a009
59291527 111971 1 None 2 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1sccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298333 111971 1 None 2 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1sccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
25006208 112327 0 None -1 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 5.0 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cc(Cl)cc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298763 112327 0 None -1 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 5.0 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cc(Cl)cc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307197 112327 0 None -1 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 5.0 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cc(Cl)cc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
367 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
5487427 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
8592 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
CHEMBL1900528 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
CHEMBL3305968 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
CHEMBL4650755 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
DB01409 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
CHEMBL5074216 212544 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074599 212548 0 None 2 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5091461 213535 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)cc1OC 10.1021/acs.jmedchem.1c00204
164613832 183956 0 None 3 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4847910 183956 0 None 3 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164615119 184390 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4854091 184390 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164622948 185522 0 None -1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 911 18 5 9 8.7 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)N(CCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)Cc4ccccc4)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4871702 185522 0 None -1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 911 18 5 9 8.7 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)N(CCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)Cc4ccccc4)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164615119 184390 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL4854091 184390 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
168280960 190254 0 None -6 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5184455 190254 0 None -6 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
10291366 140168 0 None 4 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 1 3 3.0 CO[C@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL381623 140168 0 None 4 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 1 3 3.0 CO[C@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
9874175 58230 1 None 34 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
CHEMBL1683934 58230 1 None 34 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
16065403 67593 16 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910856 67593 16 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
71452756 79131 0 None -4 4 Human 9.9 pKi = 9.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
CHEMBL2114068 79131 0 None -4 4 Human 9.9 pKi = 9.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
10291366 140168 0 None 4 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 347 3 1 3 3.0 CO[C@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL381623 140168 0 None 4 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 347 3 1 3 3.0 CO[C@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
11691950 12653 0 None 2 3 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187853 12653 0 None 2 3 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL524097 12653 0 None 2 3 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
316 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
317 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
71183 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
CHEMBL3140030 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
CHEMBL376897 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
DB00462 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
316 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
317 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
71183 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
CHEMBL3140030 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
CHEMBL376897 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
DB00462 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
316 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
317 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
71183 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
CHEMBL3140030 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
CHEMBL376897 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
DB00462 2793 14 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
367 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
5487427 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
8592 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL1900528 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL3305968 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL4650755 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
DB01409 3764 8 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
10348864 58231 0 None 147 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 616 18 5 7 6.7 O=CNc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1016/j.bmcl.2011.01.043
CHEMBL1683935 58231 0 None 147 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 616 18 5 7 6.7 O=CNc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1016/j.bmcl.2011.01.043
10054373 58232 0 None 436 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 603 17 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683936 58232 0 None 436 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 603 17 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)CC1 10.1016/j.bmcl.2011.01.043
9798900 62806 0 None 2 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL1779047 62806 0 None 2 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL1789446 62806 0 None 2 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
316 2793 14 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
317 2793 14 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
71183 2793 14 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3140030 2793 14 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL376897 2793 14 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB00462 2793 14 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL5075132 212588 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)cc2F)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076558 212677 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076637 212683 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5077161 212715 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)cc2)cc1OC 10.1021/acs.jmedchem.1c00204
164617389 184288 0 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 682 17 5 8 6.2 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4852629 184288 0 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 682 17 5 8 6.2 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
168296356 191887 0 None -3 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 751 16 5 12 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5208957 191887 0 None -3 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 751 16 5 12 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
44232952 102908 0 None -3 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084650 102908 0 None -3 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
118737348 118545 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426691 118545 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
688566 194210 21 None 1 3 Rat 9.8 pKi = 9.8 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 337 4 1 4 2.6 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm00059a009
CHEMBL558910 194210 21 None 1 3 Rat 9.8 pKi = 9.8 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 337 4 1 4 2.6 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm00059a009
10274019 202548 0 None -2 5 Human 9.8 pKi = 9.8 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 3 6.0 COc1ccc([S+]([O-])c2ccc(C(C)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL71124 202548 0 None -2 5 Human 9.8 pKi = 9.8 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 3 6.0 COc1ccc([S+]([O-])c2ccc(C(C)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
11431874 73932 0 None -1 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membraneDisplacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membrane
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023762 73932 0 None -1 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membraneDisplacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membrane
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023764 73932 0 None -1 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membraneDisplacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membrane
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
86765983 145281 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 342 4 0 2 4.1 C[C@@](C(=O)O[C@@H]1CC2CCC1[N+]2(C)C)(c1ccccc1)C1CCCC1 nan
CHEMBL3917058 145281 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 342 4 0 2 4.1 C[C@@](C(=O)O[C@@H]1CC2CCC1[N+]2(C)C)(c1ccccc1)C1CCCC1 nan
16065407 67602 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2F)C1 10.1021/jm200884j
CHEMBL1910865 67602 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2F)C1 10.1021/jm200884j
156015976 177747 0 None 2 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 337 3 1 2 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccccc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4644192 177747 0 None 2 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 337 3 1 2 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccccc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4651109 177747 0 None 2 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 337 3 1 2 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccccc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
16086001 138684 0 None 117 5 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 716 11 2 5 5.0 O=C(NCC1CCN(CC2CC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL378772 138684 0 None 117 5 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 716 11 2 5 5.0 O=C(NCC1CCN(CC2CC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
10326800 58233 1 None 70 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683938 58233 1 None 70 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
25897919 55363 11 None -2 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmc.2014.04.031
657309 55363 11 None -2 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmc.2014.04.031
CHEMBL1464005 55363 11 None -2 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmc.2014.04.031
CHEMBL1621597 55363 11 None -2 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmc.2014.04.031
16034837 67588 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910851 67588 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
53372934 128778 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670826 128778 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
53372936 128779 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670827 128779 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
59291413 112290 0 None -1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298589 112290 0 None -1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305767 112290 0 None -1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
16086063 80150 0 None 57 5 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 744 11 2 5 5.8 O=C(NCC1CCN(CC2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL214898 80150 0 None 57 5 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 744 11 2 5 5.8 O=C(NCC1CCN(CC2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL5076266 212653 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(F)c(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076445 212670 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076558 212677 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5084383 213140 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3cccc(F)c3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5090464 213490 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1ccc(CN(C(=O)O[C@H]2CN3CCC2CC3)c2ccccc2F)s1 10.1021/acs.jmedchem.1c00204
168290830 191358 0 None -7 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 790 17 5 11 6.0 COc1cc(C(=O)OCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
CHEMBL5200887 191358 0 None -7 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 790 17 5 11 6.0 COc1cc(C(=O)OCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
367 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
5487427 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
8592 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
CHEMBL1900528 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
CHEMBL3305968 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
CHEMBL4650755 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
DB01409 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
10269503 166527 0 None 7 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL428962 166527 0 None 7 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
10327462 118542 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl 10.1021/jm501915g
CHEMBL3426688 118542 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl 10.1021/jm501915g
10327461 118544 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c(Cl)c1 10.1021/jm501915g
CHEMBL3426690 118544 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c(Cl)c1 10.1021/jm501915g
118737357 118559 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 703 12 5 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426705 118559 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 703 12 5 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
44406573 72628 0 None 6 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#CC(O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200693 72628 0 None 6 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#CC(O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
59291259 111981 1 None 1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.6 O=C(Nc1ncsc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298591 111981 1 None 1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.6 O=C(Nc1ncsc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
367 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
5487427 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
8592 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
CHEMBL1900528 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
CHEMBL3305968 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
CHEMBL4650755 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
DB01409 3764 8 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
59548051 124699 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645292 124699 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548124 124701 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645294 124701 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548120 124703 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645296 124703 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548119 124706 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645299 124706 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548129 124709 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645301 124709 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843902 124710 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645302 124710 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548098 124711 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645303 124711 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548123 124712 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645304 124712 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548095 124715 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645307 124715 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548136 124718 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645310 124718 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843740 124720 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645312 124720 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843734 124724 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645316 124724 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548091 124725 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645317 124725 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548077 124727 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645319 124727 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548132 124729 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645320 124729 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548118 124730 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645321 124730 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548139 124732 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645323 124732 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548058 124740 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 124740 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548052 124746 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645337 124746 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548072 124748 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645339 124748 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548114 124754 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645344 124754 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548116 124757 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645347 124757 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548085 124759 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645349 124759 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548078 124763 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645353 124763 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548082 124764 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645354 124764 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548137 124767 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645357 124767 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548105 124771 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 124771 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
118405900 153134 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 852 15 6 10 7.4 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3981221 153134 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 852 15 6 10 7.4 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548051 124699 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645292 124699 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548124 124701 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645294 124701 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548120 124703 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645296 124703 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548087 124704 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 872 15 6 10 7.7 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645297 124704 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 872 15 6 10 7.7 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548119 124706 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645299 124706 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548129 124709 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645301 124709 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843902 124710 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645302 124710 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548098 124711 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645303 124711 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548123 124712 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645304 124712 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548095 124715 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645307 124715 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548136 124718 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645310 124718 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843740 124720 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645312 124720 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843734 124724 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645316 124724 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548091 124725 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645317 124725 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548077 124727 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645319 124727 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548132 124729 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645320 124729 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548118 124730 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645321 124730 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548139 124732 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645323 124732 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548058 124740 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 124740 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548052 124746 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645337 124746 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548072 124748 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645339 124748 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548114 124754 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645344 124754 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548116 124757 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645347 124757 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548085 124759 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645349 124759 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548115 124760 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645350 124760 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548078 124763 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645353 124763 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548082 124764 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645354 124764 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548137 124767 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645357 124767 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548105 124771 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 124771 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548051 124699 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645292 124699 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548124 124701 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645294 124701 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548120 124703 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645296 124703 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548087 124704 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 872 15 6 10 7.7 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645297 124704 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 872 15 6 10 7.7 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548119 124706 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645299 124706 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548129 124709 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645301 124709 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843902 124710 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645302 124710 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548098 124711 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645303 124711 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548123 124712 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645304 124712 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548095 124715 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645307 124715 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548136 124718 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645310 124718 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843740 124720 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645312 124720 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843734 124724 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645316 124724 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548091 124725 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645317 124725 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548077 124727 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645319 124727 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548132 124729 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645320 124729 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548118 124730 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645321 124730 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548139 124732 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645323 124732 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548058 124740 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 124740 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548052 124746 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645337 124746 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548072 124748 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645339 124748 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548114 124754 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645344 124754 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548116 124757 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645347 124757 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548085 124759 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645349 124759 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548115 124760 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645350 124760 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548078 124763 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645353 124763 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548082 124764 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645354 124764 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548137 124767 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645357 124767 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548105 124771 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 124771 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
16065137 67587 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910850 67587 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
59291461 112278 0 None 2 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1cscc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298334 112278 0 None 2 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1cscc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305613 112278 0 None 2 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1cscc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
25897919 55363 11 None 1 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
657309 55363 11 None 1 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1464005 55363 11 None 1 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1621597 55363 11 None 1 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
44431393 87596 0 None -1 3 Human 9.7 pKi = 9.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 402 6 1 5 3.5 CN(C)C1(CNCCC2CCOCC2)COc2cc(Cl)c(Cl)cc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234440 87596 0 None -1 3 Human 9.7 pKi = 9.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 402 6 1 5 3.5 CN(C)C1(CNCCC2CCOCC2)COc2cc(Cl)c(Cl)cc2OC1 10.1016/j.bmcl.2006.11.058
1734 116 8 None 1 12 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
307 116 8 None 1 12 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
CHEMBL168067 116 8 None 1 12 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
53372938 128780 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 128780 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
138680032 177727 0 None 3 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 355 3 1 2 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4639307 177727 0 None 3 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 355 3 1 2 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650981 177727 0 None 3 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 355 3 1 2 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
49800047 14334 1 None -2 5 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
CHEMBL1201024 14334 1 None -2 5 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
CHEMBL1201268 14334 1 None -2 5 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
10919522 78508 0 None 3 5 Human 9.6 pKi = 9.6 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 688 11 1 4 6.8 O=C(NC[C@H]1CCCN(CC2CCCCC2)C1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm010480k
CHEMBL2112957 78508 0 None 3 5 Human 9.6 pKi = 9.6 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 688 11 1 4 6.8 O=C(NC[C@H]1CCCN(CC2CCCCC2)C1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm010480k
9946298 72482 0 None 3 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 CO[C@]1(C#C[C@@](O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200171 72482 0 None 3 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 CO[C@]1(C#C[C@@](O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406597 72564 0 None 12 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 339 3 1 3 3.2 COC1(C#CC(O)(c2ccccc2)C2CCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200432 72564 0 None 12 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 339 3 1 3 3.2 COC1(C#CC(O)(c2ccccc2)C2CCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
59291513 112320 0 None 1 3 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1cccc(Cl)c1)C2 10.1016/j.bmc.2014.04.031
CHEMBL3298598 112320 0 None 1 3 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1cccc(Cl)c1)C2 10.1016/j.bmc.2014.04.031
CHEMBL3307127 112320 0 None 1 3 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1cccc(Cl)c1)C2 10.1016/j.bmc.2014.04.031
138710679 177601 0 None 2 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 396 4 2 3 5.3 O=C(Nc1ccc(F)cc1-c1ccc(Cl)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4649201 177601 0 None 2 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 396 4 2 3 5.3 O=C(Nc1ccc(F)cc1-c1ccc(Cl)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL5086393 213253 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5090179 213473 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1cc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)ccc1OC(F)F 10.1021/acs.jmedchem.1c00204
71113213 183867 0 None -1 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4846536 183867 0 None -1 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164621790 185210 0 None -5 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 849 17 5 9 7.6 CCN(CCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C(=O)c1ccc(COc2cccc(-c3ccc([C@@H](NC(=O)O[C@H]4CN5CCC4CC5)c4ccccc4)cc3)c2)cc1 10.1016/j.bmcl.2021.127975
CHEMBL4866806 185210 0 None -5 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 849 17 5 9 7.6 CCN(CCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C(=O)c1ccc(COc2cccc(-c3ccc([C@@H](NC(=O)O[C@H]4CN5CCC4CC5)c4ccccc4)cc3)c2)cc1 10.1016/j.bmcl.2021.127975
154417 92828 57 None -2 10 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2013.12.024
CHEMBL2449003 92828 57 None -2 10 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2013.12.024
127044 78500 1 None 2 3 Rat 9.6 pKi = 9.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 427 5 1 4 2.9 O=C(OC1CN2CCC1CC2)C(O)(CC=CI)c1ccccc1 10.1021/jm00059a009
CHEMBL2112942 78500 1 None 2 3 Rat 9.6 pKi = 9.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 427 5 1 4 2.9 O=C(OC1CN2CCC1CC2)C(O)(CC=CI)c1ccccc1 10.1021/jm00059a009
154417 92828 57 None -2 10 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2013.12.024
CHEMBL2449003 92828 57 None -2 10 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2013.12.024
1201549 590 22 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 590 22 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 590 22 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 590 22 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 590 22 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 590 22 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
54580129 61466 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 786 21 6 8 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773197 61466 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 786 21 6 8 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
25897919 55363 11 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
657309 55363 11 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1464005 55363 11 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1621597 55363 11 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
44610056 123473 0 None -2 5 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629360 123473 0 None -2 5 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
16086059 80363 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm301774u
CHEMBL215180 80363 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm301774u
367 3764 8 None -30 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
5487427 3764 8 None -30 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
8592 3764 8 None -30 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
CHEMBL1900528 3764 8 None -30 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
CHEMBL3305968 3764 8 None -30 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
CHEMBL4650755 3764 8 None -30 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
DB01409 3764 8 None -30 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
16086059 80363 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215180 80363 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
70843738 124721 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645313 124721 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548128 124738 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645329 124738 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548080 124743 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645334 124743 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548088 124747 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645338 124747 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548059 124750 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645340 124750 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548084 124752 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645342 124752 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
118405092 149720 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 848 15 5 8 8.9 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](C)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3952427 149720 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 848 15 5 8 8.9 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](C)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548106 124714 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645306 124714 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843738 124721 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645313 124721 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548128 124738 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645329 124738 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548080 124743 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645334 124743 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548088 124747 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645338 124747 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548059 124750 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645340 124750 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548084 124752 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645342 124752 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548106 124714 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645306 124714 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843738 124721 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645313 124721 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548128 124738 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645329 124738 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548080 124743 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645334 124743 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548088 124747 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645338 124747 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548059 124750 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645340 124750 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548084 124752 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645342 124752 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
53239456 61489 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773267 61489 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
11039424 78506 1 None 45 5 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 622 14 3 4 5.4 O=C(CCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112955 78506 1 None 45 5 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 622 14 3 4 5.4 O=C(CCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
53239456 61489 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2015.10.008
CHEMBL1773267 61489 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2015.10.008
72712268 105977 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 1 6 2.4 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(CO)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3091670 105977 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 1 6 2.4 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(CO)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3140032 105977 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 1 6 2.4 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(CO)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL5076680 212687 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)Cc2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)cc2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5081816 212998 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5084829 213164 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None CCOc1cc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)ccc1OC(F)F 10.1021/acs.jmedchem.1c00204
CHEMBL5085717 213211 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None CC(C)Oc1cc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)ccc1OC(F)F 10.1021/acs.jmedchem.1c00204
CHEMBL5086769 213275 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3cccc(O)c3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5088742 213401 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
71113309 184999 0 None -19 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(NC(c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4863525 184999 0 None -19 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(NC(c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
71093373 191826 0 None -7 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(NC(c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5208201 191826 0 None -7 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(NC(c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
25897919 55363 11 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2008.03.024
657309 55363 11 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2008.03.024
CHEMBL1464005 55363 11 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2008.03.024
CHEMBL1621597 55363 11 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2008.03.024
25010559 96321 0 None 10 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 381 3 1 3 4.3 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL264676 96321 0 None 10 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 381 3 1 3 4.3 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
10109563 157994 0 None 7 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 367 3 1 3 4.0 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL409151 157994 0 None 7 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 367 3 1 3 4.0 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
118737352 118550 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 6 9 6.1 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426696 118550 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 6 9 6.1 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
10394806 118552 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 681 12 6 8 5.3 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)N[C@H]1CC[C@H](CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
CHEMBL3426698 118552 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 681 12 6 8 5.3 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)N[C@H]1CC[C@H](CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
118737356 118557 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 753 13 5 9 6.5 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426703 118557 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 753 13 5 9 6.5 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
16086059 80363 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215180 80363 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
44406662 165730 0 None 12 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 366 3 1 4 2.6 COC1(C#CC(O)(c2ccccc2)c2ccc(F)nc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL427013 165730 0 None 12 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 366 3 1 4 2.6 COC1(C#CC(O)(c2ccccc2)c2ccc(F)nc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
9986442 58229 0 None 10 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 626 15 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683933 58229 0 None 10 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 626 15 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
16116085 11741 0 None -3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1182201 11741 0 None -3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL219786 11741 0 None -3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
122194236 123467 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 362 5 1 5 2.9 CN1CCC(Cn2cnc(C(O)(c3ccccc3)c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.10.008
CHEMBL3629354 123467 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 362 5 1 5 2.9 CN1CCC(Cn2cnc(C(O)(c3ccccc3)c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.10.008
155157200 177364 0 None 1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 340 3 1 3 4.1 O=C(Nc1ccc(F)cc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4645543 177364 0 None 1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 340 3 1 3 4.1 O=C(Nc1ccc(F)cc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
156015097 176978 0 None 1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4640324 176978 0 None 1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
10567858 177305 0 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 322 3 1 3 4.0 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4644670 177305 0 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 322 3 1 3 4.0 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
59291327 112319 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.6 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1ccccc1)C2 10.1016/j.bmc.2014.04.031
CHEMBL3298597 112319 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.6 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1ccccc1)C2 10.1016/j.bmc.2014.04.031
CHEMBL3307126 112319 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.6 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1ccccc1)C2 10.1016/j.bmc.2014.04.031
71454563 79246 0 None -6 4 Human 9.4 pKi = 9.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
CHEMBL2115128 79246 0 None -6 4 Human 9.4 pKi = 9.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
90666101 108844 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 666 18 5 8 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219031 108844 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 666 18 5 8 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1039/C1MD00140J
156021744 177540 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4648071 177540 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
16086066 138705 0 None 134 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL378872 138705 0 None 134 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
16086060 168377 0 None 100 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL438822 168377 0 None 100 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
54583092 61467 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 695 19 6 7 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3cc(O)cc(O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773198 61467 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 695 19 6 7 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3cc(O)cc(O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL5076535 212674 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076558 212677 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5087564 213334 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(NC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
164616287 184413 0 None -3 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 668 16 5 8 5.8 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4854418 184413 0 None -3 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 668 16 5 8 5.8 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164627621 185744 0 None -15 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 640 14 5 8 5.0 O=C(NC(c1ccccc1)c1cccc(OCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4874819 185744 0 None -15 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 640 14 5 8 5.0 O=C(NC(c1ccccc1)c1cccc(OCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
44406481 72530 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200319 72530 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
1734 116 8 None 1 12 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
307 116 8 None 1 12 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL168067 116 8 None 1 12 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
134272501 176007 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4483083 176007 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597500 176007 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
70843737 124723 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645315 124723 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548060 124745 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645336 124745 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843737 124723 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645315 124723 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548060 124745 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645336 124745 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843737 124723 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645315 124723 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548060 124745 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645336 124745 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
1734 116 8 None 1 12 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
307 116 8 None 1 12 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
CHEMBL168067 116 8 None 1 12 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
174174 519 46 None -2 14 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
260 519 46 None -2 14 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
320 519 46 None -2 14 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
CHEMBL517712 519 46 None -2 14 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
DB00572 519 46 None -2 14 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
1734 116 8 None 1 12 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm401895u
307 116 8 None 1 12 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm401895u
CHEMBL168067 116 8 None 1 12 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm401895u
134272452 176100 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(OC1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4448944 176100 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(OC1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4598232 176100 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(OC1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
11223598 106043 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084413 106043 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140264 106043 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11061341 78509 0 None 23 5 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 662 13 2 4 6.3 O=C(CCNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112958 78509 0 None 23 5 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 662 13 2 4 6.3 O=C(CCNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
10567858 177305 0 None -1 6 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptorDisplacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptor
ChEMBL 322 3 1 3 4.0 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4644670 177305 0 None -1 6 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptorDisplacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptor
ChEMBL 322 3 1 3 4.0 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
156013794 176702 0 None 3 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 310 4 2 3 3.9 O=C(Nc1ccccc1-c1ccccc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636302 176702 0 None 3 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 310 4 2 3 3.9 O=C(Nc1ccccc1-c1ccccc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
15599352 108136 0 None -2 2 Rat 9.3 pKi = 9.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL320611 108136 0 None -2 2 Rat 9.3 pKi = 9.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
9867847 202555 0 None -2 4 Human 9.3 pKi = 9.3 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 439 6 0 4 5.6 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
CHEMBL71147 202555 0 None -2 4 Human 9.3 pKi = 9.3 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 439 6 0 4 5.6 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
9867847 202555 0 None -2 4 Human 9.3 pKi = 9.3 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 439 6 0 4 5.6 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00457-1
CHEMBL71147 202555 0 None -2 4 Human 9.3 pKi = 9.3 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 439 6 0 4 5.6 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00457-1
16085999 79882 0 None 60 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 676 10 3 5 4.3 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL214029 79882 0 None 60 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 676 10 3 5 4.3 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
174174 519 46 None -2 14 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
260 519 46 None -2 14 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
320 519 46 None -2 14 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
CHEMBL517712 519 46 None -2 14 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
DB00572 519 46 None -2 14 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
CHEMBL5076886 212696 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3C[C@H]4CC[C@H](C3)N4C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5078006 212757 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5085166 213180 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccn3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
118737351 118549 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 6 9 6.1 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1C 10.1021/jm501915g
CHEMBL3426695 118549 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 6 9 6.1 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1C 10.1021/jm501915g
140844407 176058 0 None -4 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3ccc(Cl)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4519930 176058 0 None -4 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3ccc(Cl)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597916 176058 0 None -4 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3ccc(Cl)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
16086064 79550 0 None 93 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 730 10 2 5 5.6 O=C(NCC1CCN(C2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL212645 79550 0 None 93 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 730 10 2 5 5.6 O=C(NCC1CCN(C2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
16086000 79946 0 None 79 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 676 9 2 5 4.2 CN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
CHEMBL214342 79946 0 None 79 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 676 9 2 5 4.2 CN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
71450948 79126 0 None -1 2 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1C[C@H]2OC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00090a006
CHEMBL2114060 79126 0 None -1 2 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1C[C@H]2OC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00090a006
53317170 58221 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 409 10 2 4 5.3 NCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683925 58221 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 409 10 2 4 5.3 NCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
138711343 177250 0 None 1 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 408 3 1 3 5.4 O=C(Nc1ccc(F)cc1-c1ccc(Cl)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4643867 177250 0 None 1 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 408 3 1 3 5.4 O=C(Nc1ccc(F)cc1-c1ccc(Cl)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
174174 519 46 None -2 14 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2018.12.022
260 519 46 None -2 14 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2018.12.022
320 519 46 None -2 14 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2018.12.022
CHEMBL517712 519 46 None -2 14 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2018.12.022
DB00572 519 46 None -2 14 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2018.12.022
16086062 80379 0 None 58 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 730 11 2 5 5.4 O=C(NCC1CCN(CC2CCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215189 80379 0 None 58 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 730 11 2 5 5.4 O=C(NCC1CCN(CC2CCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
71449175 79242 0 None 1 2 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1C[C@@H]2OC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00090a006
CHEMBL2115124 79242 0 None 1 2 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1C[C@@H]2OC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00090a006
3028236 102126 1 None 36 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 340 9 0 2 4.2 CC[N+](CC)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377383 102126 1 None 36 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 340 9 0 2 4.2 CC[N+](CC)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL3041159 102126 1 None 36 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 340 9 0 2 4.2 CC[N+](CC)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
11434515 259 3 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
11519741 259 3 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
4484 259 3 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
7449 259 3 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
CHEMBL1194325 259 3 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
DB08897 259 3 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
2028 2931 77 None 1 11 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 2931 77 None 1 11 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 2931 77 None 1 11 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 2931 77 None 1 11 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 2931 77 None 1 11 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
16115945 12191 0 None -2 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1184886 12191 0 None -2 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL376057 12191 0 None -2 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
9880462 72559 0 None 39 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 327 5 1 3 3.2 CCCCC(O)(C#CC1(OC)CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2005.09.079
CHEMBL200416 72559 0 None 39 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 327 5 1 3 3.2 CCCCC(O)(C#CC1(OC)CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2005.09.079
138711325 177322 0 None 3 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 328 4 2 3 4.0 O=C(Nc1ccc(F)cc1-c1ccccc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4644852 177322 0 None 3 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 328 4 2 3 4.0 O=C(Nc1ccc(F)cc1-c1ccccc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL5077424 212727 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C)C(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086895 213281 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1cccc(CNC(C(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.1c00204
CHEMBL5094110 213696 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(S(=O)(=O)NC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
118737349 118546 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 739 13 6 9 6.4 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1Cl 10.1021/jm501915g
CHEMBL3426692 118546 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 739 13 6 9 6.4 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1Cl 10.1021/jm501915g
10439505 118553 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 675 12 6 8 5.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCNC(=O)c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)CC1 10.1021/jm501915g
CHEMBL3426699 118553 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 675 12 6 8 5.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCNC(=O)c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)CC1 10.1021/jm501915g
87142783 118558 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426704 118558 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
54583100 61486 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 731 21 5 8 7.4 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773264 61486 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 731 21 5 8 7.4 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
155619955 176951 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 368 3 1 4 3.7 CN1[C@H]2C[C@@H](OC(=O)Nc3ccc(F)cc3-c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/acs.jmedchem.0c00297
CHEMBL4639938 176951 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 368 3 1 4 3.7 CN1[C@H]2C[C@@H](OC(=O)Nc3ccc(F)cc3-c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/acs.jmedchem.0c00297
134272442 175914 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 4 4.9 O=C(OC1C[N+]2(CCSc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4457734 175914 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 4 4.9 O=C(OC1C[N+]2(CCSc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596671 175914 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 4 4.9 O=C(OC1C[N+]2(CCSc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
44420795 11745 0 None 7 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 426 6 1 1 4.4 C[N+]1(CCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL1182222 11745 0 None 7 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 426 6 1 1 4.4 C[N+]1(CCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL223055 11745 0 None 7 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 426 6 1 1 4.4 C[N+]1(CCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
1734 116 8 None 1 12 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2007.09.003
307 116 8 None 1 12 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2007.09.003
CHEMBL168067 116 8 None 1 12 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2007.09.003
16125331 136439 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 440 7 1 1 4.8 C[N+]1(CCCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL374452 136439 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 440 7 1 1 4.8 C[N+]1(CCCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
24764458 108854 2 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 716 18 6 9 6.9 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219042 108854 2 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 716 18 6 9 6.9 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
122194235 123466 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 690 16 6 8 7.3 O=C(Nc1ccccc1-c1ccc(O)c(Cl)c1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2015.10.008
CHEMBL3629353 123466 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 690 16 6 8 7.3 O=C(Nc1ccccc1-c1ccc(O)c(Cl)c1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2015.10.008
10438748 58228 0 None 13 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 612 14 5 7 6.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683932 58228 0 None 13 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 612 14 5 7 6.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
319 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
16116083 12190 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL1184884 12190 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL375969 12190 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
53323772 58223 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 437 12 2 4 6.1 NCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683927 58223 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 437 12 2 4 6.1 NCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16664965 84478 0 None 28 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 462 6 1 1 4.7 C[N+]1(CCc2ccccc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL223668 84478 0 None 28 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 462 6 1 1 4.7 C[N+]1(CCc2ccccc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
11828362 78510 0 None 39 5 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 636 15 3 4 5.8 O=C(CCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112959 78510 0 None 39 5 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 636 15 3 4 5.8 O=C(CCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
24876564 61452 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 668 20 5 7 7.5 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773074 61452 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 668 20 5 7 7.5 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
2028 2931 77 None 1 11 Human 9.1 pKi = 9.1 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2006.11.058
359 2931 77 None 1 11 Human 9.1 pKi = 9.1 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2006.11.058
4634 2931 77 None 1 11 Human 9.1 pKi = 9.1 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2006.11.058
CHEMBL1231 2931 77 None 1 11 Human 9.1 pKi = 9.1 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2006.11.058
DB01062 2931 77 None 1 11 Human 9.1 pKi = 9.1 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2006.11.058
44406686 140380 0 None 3 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 366 3 1 4 2.6 COC1(C#CC(O)(c2ccccc2)c2cccnc2F)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL382213 140380 0 None 3 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 366 3 1 4 2.6 COC1(C#CC(O)(c2ccccc2)c2cccnc2F)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
10199963 140784 0 None 6 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 383 3 1 3 3.3 CO[C@]1(C#CC(O)(c2cccc(F)c2)c2cccc(F)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL383389 140784 0 None 6 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 383 3 1 3 3.3 CO[C@]1(C#CC(O)(c2cccc(F)c2)c2cccc(F)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
25897919 55363 11 None 1 8 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/acs.jmedchem.1c00204
657309 55363 11 None 1 8 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/acs.jmedchem.1c00204
CHEMBL1464005 55363 11 None 1 8 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/acs.jmedchem.1c00204
CHEMBL1621597 55363 11 None 1 8 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/acs.jmedchem.1c00204
CHEMBL5078680 212807 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1cccc(NC(C(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.1c00204
CHEMBL5086272 213248 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3nccs3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
168279881 190268 0 None -15 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5184598 190268 0 None -15 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
86720814 191339 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc([C@@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
CHEMBL5200448 191339 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc([C@@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
118719922 115275 0 None 1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 115275 0 None 1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
118737355 118556 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 5 8 5.5 CN(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)C(=O)c1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
CHEMBL3426702 118556 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 5 8 5.5 CN(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)C(=O)c1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
44318782 204413 0 None 63 2 Human 9.1 pKi = 9.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 482 5 0 2 6.4 O=C(c1ccc(Cl)cc1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85996 204413 0 None 63 2 Human 9.1 pKi = 9.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 482 5 0 2 6.4 O=C(c1ccc(Cl)cc1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
174174 519 46 None -1 14 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
260 519 46 None -1 14 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
320 519 46 None -1 14 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
CHEMBL517712 519 46 None -1 14 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
DB00572 519 46 None -1 14 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
59548053 124765 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645355 124765 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548053 124765 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645355 124765 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548053 124765 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645355 124765 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
11693 1797 12 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
3494 1797 12 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
4302 1797 12 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
7459 1797 12 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
CHEMBL1201335 1797 12 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
DB00986 1797 12 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
11155732 10447 14 None -2 3 Rat 9.1 pKi = 9.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
CHEMBL1169543 10447 14 None -2 3 Rat 9.1 pKi = 9.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
9874175 58230 1 None 34 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1039/C1MD00140J
CHEMBL1683934 58230 1 None 34 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1039/C1MD00140J
25897919 55363 11 None 1 8 Human 9.1 pKi = 9.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
657309 55363 11 None 1 8 Human 9.1 pKi = 9.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
CHEMBL1464005 55363 11 None 1 8 Human 9.1 pKi = 9.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
CHEMBL1621597 55363 11 None 1 8 Human 9.1 pKi = 9.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
319 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
321 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
444031 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
784 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
CHEMBL1346 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
DB00496 1297 39 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
152278786 182170 0 None 1 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assay
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 182170 0 None 1 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assay
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
75167447 177711 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4634230 177711 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650933 177711 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
134272561 175853 0 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 442 7 1 3 4.3 O=C(OC1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4540604 175853 0 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 442 7 1 3 4.3 O=C(OC1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596189 175853 0 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 442 7 1 3 4.3 O=C(OC1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
145148382 176040 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
CHEMBL4590868 176040 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
CHEMBL4597793 176040 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
56667296 176067 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 472 9 1 4 4.5 O=C(OC1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4461243 176067 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 472 9 1 4 4.5 O=C(OC1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597972 176067 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 472 9 1 4 4.5 O=C(OC1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
16115951 141111 0 None 1 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL385328 141111 0 None 1 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
46188794 177744 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4645580 177744 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651099 177744 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
174174 519 46 None -2 14 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
260 519 46 None -2 14 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
320 519 46 None -2 14 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
CHEMBL517712 519 46 None -2 14 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
DB00572 519 46 None -2 14 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
156015287 177001 0 None 3 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 364 4 2 3 4.3 O=C(Nc1ccccc1-c1cc(F)c(F)c(F)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640544 177001 0 None 3 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 364 4 2 3 4.3 O=C(Nc1ccccc1-c1cc(F)c(F)c(F)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
16115947 11744 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1182214 11744 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL222259 11744 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
16086061 79808 0 None 99 5 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 690 10 2 5 4.6 CCN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
CHEMBL213709 79808 0 None 99 5 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 690 10 2 5 4.6 CCN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
3042 1386 31 None -1 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1386 31 None -1 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1386 31 None -1 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1386 31 None -1 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1386 31 None -1 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
59291421 112280 0 None -1 3 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1ncsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298592 112280 0 None -1 3 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1ncsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305620 112280 0 None -1 3 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1ncsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
2028 2931 77 None -1 11 Rat 9.0 pKi = 9.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.02.036
359 2931 77 None -1 11 Rat 9.0 pKi = 9.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.02.036
4634 2931 77 None -1 11 Rat 9.0 pKi = 9.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.02.036
CHEMBL1231 2931 77 None -1 11 Rat 9.0 pKi = 9.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.02.036
DB01062 2931 77 None -1 11 Rat 9.0 pKi = 9.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.02.036
156014269 176642 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4635500 176642 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
16125370 84223 0 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 2 5.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL222387 84223 0 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 2 5.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCCN(Cc2ccccc2)CC1 10.1021/jm061159a
154417 92828 57 None -1 10 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cells
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2007.12.051
CHEMBL2449003 92828 57 None -1 10 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cells
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2007.12.051
10180872 102654 0 None 1 4 Human 9.0 pKi = 9.0 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 426 6 0 4 4.9 COc1ccc([S+]([O-])c2ccc(C(C)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL307810 102654 0 None 1 4 Human 9.0 pKi = 9.0 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 426 6 0 4 4.9 COc1ccc([S+]([O-])c2ccc(C(C)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
54582151 61488 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 711 24 5 8 7.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773266 61488 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 711 24 5 8 7.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
11767229 78507 0 None 30 5 Human 9.0 pKi = 9 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 607 15 2 3 7.5 O=C(CCCCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112956 78507 0 None 30 5 Human 9.0 pKi = 9 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 607 15 2 3 7.5 O=C(CCCCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
44406598 72679 0 None 6 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 3 1 3 2.8 COC1(C#CC(O)(c2ccccc2)C2CCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200957 72679 0 None 6 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 3 1 3 2.8 COC1(C#CC(O)(c2ccccc2)C2CCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406690 74644 0 None 1 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 COC1(C#CC(O)(c2ccccc2)c2cncnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL203249 74644 0 None 1 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 COC1(C#CC(O)(c2ccccc2)c2cncnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406268 140265 0 None 19 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 383 3 1 3 3.3 CO[C@]1(C#CC(O)(c2ccc(F)cc2)c2ccc(F)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL381878 140265 0 None 19 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 383 3 1 3 3.3 CO[C@]1(C#CC(O)(c2ccc(F)cc2)c2ccc(F)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
90198269 189794 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 492 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OC[C@H]2CC[C@H](C(=O)O)CC2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5177499 189794 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 492 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OC[C@H]2CC[C@H](C(=O)O)CC2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
138711318 177546 0 None 4 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 346 4 2 3 4.2 O=C(Nc1ccc(F)cc1-c1ccc(F)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4648196 177546 0 None 4 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 346 4 2 3 4.2 O=C(Nc1ccc(F)cc1-c1ccc(F)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
118737358 118560 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 13 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1021/jm501915g
CHEMBL3426706 118560 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 13 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1021/jm501915g
10049361 204401 0 None 10 2 Human 9.0 pKi = 9 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 448 5 0 2 5.8 O=C(c1ccccc1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85892 204401 0 None 10 2 Human 9.0 pKi = 9 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 448 5 0 2 5.8 O=C(c1ccccc1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
5284632 67065 8 None 1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b02100
CHEMBL1888176 67065 8 None 1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b02100
CHEMBL3084748 67065 8 None 1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b02100
16125642 141478 0 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CC[C@@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL387546 141478 0 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CC[C@@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
101882890 115276 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354069 115276 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
44308899 202308 0 None 1 3 Human 9.0 pKi = 9.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 330 5 2 3 2.7 NCCC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL69648 202308 0 None 1 3 Human 9.0 pKi = 9.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 330 5 2 3 2.7 NCCC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
59707188 108858 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219046 108858 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
90666115 108860 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 702 17 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219048 108860 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 702 17 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
77157 34701 40 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 325 4 1 4 2.6 CN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2015.10.008
CHEMBL143228 34701 40 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 325 4 1 4 2.6 CN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2015.10.008
122194237 123468 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 368 5 1 5 3.4 CN1CCC(Cn2cnc(C(O)(c3ccccc3)C3CCCCC3)n2)CC1 10.1016/j.bmcl.2015.10.008
CHEMBL3629355 123468 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 368 5 1 5 3.4 CN1CCC(Cn2cnc(C(O)(c3ccccc3)C3CCCCC3)n2)CC1 10.1016/j.bmcl.2015.10.008
138710768 177239 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 354 3 1 3 4.7 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4643643 177239 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 354 3 1 3 4.7 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
155512178 175915 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3cccc(F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4436930 175915 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3cccc(F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596672 175915 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3cccc(F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
15599355 107060 0 None -5 2 Rat 9.0 pKi = 9.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 351 4 1 4 2.9 CN1CC2CC1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL318812 107060 0 None -5 2 Rat 9.0 pKi = 9.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 351 4 1 4 2.9 CN1CC2CC1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
1734 116 8 None -2 12 Rat 8.9 pKi = 8.9 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00403-G
307 116 8 None -2 12 Rat 8.9 pKi = 8.9 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00403-G
CHEMBL168067 116 8 None -2 12 Rat 8.9 pKi = 8.9 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00403-G
1734 116 8 None -2 12 Rat 8.9 pKi = 8.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00113-8
307 116 8 None -2 12 Rat 8.9 pKi = 8.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00113-8
CHEMBL168067 116 8 None -2 12 Rat 8.9 pKi = 8.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00113-8
44308832 202116 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 364 4 2 3 2.8 NCC=C1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL68384 202116 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 364 4 2 3 2.8 NCC=C1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
16086005 138701 0 None 19 5 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 724 10 3 5 5.8 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL378859 138701 0 None 19 5 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 724 10 3 5 5.8 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL5080391 212911 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1cccc(CN(C(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.1c00204
CHEMBL5081214 212961 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1cccc(S(=O)(=O)NC(C(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.1c00204
59591029 185341 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 336 4 1 3 3.6 O=C(NC(c1ccccc1)c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4869096 185341 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 336 4 1 3 3.6 O=C(NC(c1ccccc1)c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
118737350 118548 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426694 118548 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
44319071 204300 0 None 7 2 Human 8.9 pKi = 8.9 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 404 5 0 2 5.7 O=C(c1ccccc1)N(c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL84993 204300 0 None 7 2 Human 8.9 pKi = 8.9 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 404 5 0 2 5.7 O=C(c1ccccc1)N(c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
319 1297 39 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
321 1297 39 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
444031 1297 39 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
784 1297 39 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
CHEMBL1346 1297 39 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
DB00496 1297 39 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
2028 2931 77 None 1 11 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.09.079
359 2931 77 None 1 11 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.09.079
4634 2931 77 None 1 11 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.09.079
CHEMBL1231 2931 77 None 1 11 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.09.079
DB01062 2931 77 None 1 11 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.09.079
44406521 73558 0 None 4 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2ccncc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL201933 73558 0 None 4 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2ccncc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
90666120 108866 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 728 19 6 9 6.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@@H]3[C@@H](COC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)[C@@H]3C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219053 108866 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 728 19 6 9 6.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@@H]3[C@@H](COC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)[C@@H]3C2)ccc1O 10.1039/C1MD00140J
44430454 87526 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 4 3.6 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCC1 10.1016/j.bmcl.2007.03.047
CHEMBL234099 87526 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 4 3.6 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCC1 10.1016/j.bmcl.2007.03.047
15888011 202610 0 None -1 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 302 3 2 3 2.0 NC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL71431 202610 0 None -1 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 302 3 2 3 2.0 NC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
16115799 83029 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL219825 83029 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
54586986 61485 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 780 27 6 8 8.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)CCCCCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773263 61485 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 780 27 6 8 8.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)CCCCCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
57326235 76832 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042405 76832 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079009 76832 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
44431384 148328 0 None -2 3 Human 8.8 pKi = 8.8 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 384 6 1 4 4.0 CN(C)C1(CNCCC23CC4CC(CC(C4)C2)C3)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL394137 148328 0 None -2 3 Human 8.8 pKi = 8.8 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 384 6 1 4 4.0 CN(C)C1(CNCCC23CC4CC(CC(C4)C2)C3)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
156018620 177332 0 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 396 4 2 3 5.3 O=C(Nc1ccc(F)cc1-c1cc(Cl)cc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4644999 177332 0 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 396 4 2 3 5.3 O=C(Nc1ccc(F)cc1-c1cc(Cl)cc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
155542840 175819 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 540 9 1 4 5.6 O=C(OC1C[N+]2(CCCc3ccc(OC(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4521993 175819 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 540 9 1 4 5.6 O=C(OC1C[N+]2(CCCc3ccc(OC(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4595947 175819 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 540 9 1 4 5.6 O=C(OC1C[N+]2(CCCc3ccc(OC(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
53372938 128780 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 128780 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
2028 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
359 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
4634 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
CHEMBL1231 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
DB01062 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
57326326 76825 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042553 76825 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078942 76825 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
44627858 13924 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197382 13924 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569307 13924 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
57326326 76825 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL2042553 76825 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL2078942 76825 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
72712276 105975 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 0 6 3.0 COC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
CHEMBL3091666 105975 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 0 6 3.0 COC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
CHEMBL3140016 105975 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 0 6 3.0 COC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
71093073 190992 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc(C(NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
CHEMBL5195203 190992 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc(C(NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
10484922 118543 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426689 118543 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
44319009 106453 0 None 15 2 Human 8.8 pKi = 8.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 426 5 0 2 5.2 O=C(C1CCC1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL314831 106453 0 None 15 2 Human 8.8 pKi = 8.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 426 5 0 2 5.2 O=C(C1CCC1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
53326588 58224 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 451 13 2 4 6.4 NCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683928 58224 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 451 13 2 4 6.4 NCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16086067 80905 0 None 63 5 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL215894 80905 0 None 63 5 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
16125704 84241 0 None 54 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 482 6 1 3 4.4 C[N+]1(CC(=O)c2ccsc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222450 84241 0 None 54 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 482 6 1 3 4.4 C[N+]1(CC(=O)c2ccsc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
44627853 196004 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL571121 196004 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
16115798 137352 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL376255 137352 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
15157137 99433 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 317 7 0 3 4.0 CN(C)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL286008 99433 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 317 7 0 3 4.0 CN(C)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
44308861 201834 0 None 1 3 Human 8.8 pKi = 8.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 316 4 2 3 2.3 NCC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL66400 201834 0 None 1 3 Human 8.8 pKi = 8.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 316 4 2 3 2.3 NCC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
156015047 177691 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 409 4 1 2 5.3 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
CHEMBL4645235 177691 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 409 4 1 2 5.3 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
CHEMBL4650768 177691 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 409 4 1 2 5.3 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
155520948 175855 0 None -3 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3ccc(F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4450188 175855 0 None -3 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3ccc(F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596191 175855 0 None -3 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3ccc(F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
16124706 136997 0 None 61 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 437 5 1 4 5.1 Cc1cccc(CN2CCC(N3CC(c4cccs4)(c4cccs4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL375420 136997 0 None 61 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 437 5 1 4 5.1 Cc1cccc(CN2CCC(N3CC(c4cccs4)(c4cccs4)NC3=O)CC2)c1 10.1021/jm061159a
16125587 84339 0 None 5 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 456 8 1 2 4.6 C[N+]1(CCCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL223028 84339 0 None 5 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 456 8 1 2 4.6 C[N+]1(CCCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
13567081 11130 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 320 4 0 2 4.3 C[N+](C)(C)C[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1178839 11130 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 320 4 0 2 4.3 C[N+](C)(C)C[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL45454 11130 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 320 4 0 2 4.3 C[N+](C)(C)C[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
53325045 58222 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 423 11 2 4 5.7 NCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683926 58222 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 423 11 2 4 5.7 NCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
90645361 112318 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 4.8 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(C(F)(F)F)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298601 112318 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 4.8 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(C(F)(F)F)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307123 112318 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 4.8 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(C(F)(F)F)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
16065135 67583 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910846 67583 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2)C1 10.1021/jm200884j
44443730 93599 0 None 21 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 432 6 2 3 4.7 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL248811 93599 0 None 21 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 432 6 2 3 4.7 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
16125646 136447 0 None 50 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 476 6 1 2 4.3 C[N+]1(CC(=O)c2ccccc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL374513 136447 0 None 50 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 476 6 1 2 4.3 C[N+]1(CC(=O)c2ccccc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
16125589 84275 0 None 16 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 440 6 1 2 4.1 C[N+]1(CC(=O)c2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222636 84275 0 None 16 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 440 6 1 2 4.1 C[N+]1(CC(=O)c2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
16125541 136683 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL374989 136683 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
54757332 67582 0 None 7 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 414 9 1 3 4.4 NC(=O)C(CCCN1CC[C@H](Oc2ccccc2)C1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
CHEMBL1910845 67582 0 None 7 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 414 9 1 3 4.4 NC(=O)C(CCCN1CC[C@H](Oc2ccccc2)C1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
11718536 137320 0 None 41 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 411 5 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL376000 137320 0 None 41 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 411 5 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
155530273 175777 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1cccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)c1 10.1016/j.bmc.2019.06.016
CHEMBL4463636 175777 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1cccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)c1 10.1016/j.bmc.2019.06.016
CHEMBL4595649 175777 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1cccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)c1 10.1016/j.bmc.2019.06.016
156020548 177604 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4649224 177604 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
72712476 105976 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 304 3 1 4 1.0 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3091668 105976 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 304 3 1 4 1.0 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3140031 105976 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 304 3 1 4 1.0 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
66875589 102915 0 None -3 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084662 102915 0 None -3 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
10155850 96294 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 367 3 1 3 4.0 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL264414 96294 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 367 3 1 3 4.0 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
10372836 101925 34 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3039518 101925 34 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
118737360 118562 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426708 118562 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
10789183 103888 0 None 25 2 Human 8.7 pKi = 8.7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 438 5 0 2 6.3 O=C(c1ccccc1)N(c1ccc(Cl)c(Cl)c1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL310132 103888 0 None 25 2 Human 8.7 pKi = 8.7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 438 5 0 2 6.3 O=C(c1ccccc1)N(c1ccc(Cl)c(Cl)c1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
44319342 204005 0 None 31 2 Human 8.7 pKi = 8.7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 454 5 0 3 5.8 O=C(c1cccs1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL82512 204005 0 None 31 2 Human 8.7 pKi = 8.7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 454 5 0 3 5.8 O=C(c1cccs1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
154059 3580 49 None 1 8 Rat 8.0 pKi = 8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1021/jm050099q
2457 3580 49 None 1 8 Rat 8.0 pKi = 8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1021/jm050099q
7483 3580 49 None 1 8 Rat 8.0 pKi = 8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1021/jm050099q
CHEMBL1734 3580 49 None 1 8 Rat 8.0 pKi = 8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1021/jm050099q
DB01591 3580 49 None 1 8 Rat 8.0 pKi = 8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1021/jm050099q
44406480 72499 0 None 5 2 Human 8.0 pKi = 8 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2ccccn2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200210 72499 0 None 5 2 Human 8.0 pKi = 8 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2ccccn2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL5076886 212696 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3C[C@H]4CC[C@H](C3)N4C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5081816 212998 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086393 213253 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
90666106 108849 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219036 108849 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
71113107 185998 0 None -39 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1ccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4878395 185998 0 None -39 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1ccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
372625 100678 10 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL295388 100678 10 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
372625 100678 10 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in A9 cells by scintillation counting analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in A9 cells by scintillation counting analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1039/d0md00137f
CHEMBL295388 100678 10 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in A9 cells by scintillation counting analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in A9 cells by scintillation counting analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1039/d0md00137f
372625 100678 10 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in mouse A9L cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in mouse A9L cell membranes after 60 mins by scintillation counting method
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL295388 100678 10 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in mouse A9L cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in mouse A9L cell membranes after 60 mins by scintillation counting method
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
168296296 191799 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 488 8 2 7 3.7 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cnc(C(=O)O)cn2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5207792 191799 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 488 8 2 7 3.7 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cnc(C(=O)O)cn2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
54757560 65657 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 327 3 2 5 3.0 Oc1cccc(F)c1-n1nc(OC2CCNCC2)c2ccccc21 10.1021/jm2007535
CHEMBL1836645 65657 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 327 3 2 5 3.0 Oc1cccc(F)c1-n1nc(OC2CCNCC2)c2ccccc21 10.1021/jm2007535
9969695 160341 0 None 15 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 361 4 0 3 3.7 COC(C#C[C@@]1(OC)CN2CCC1CC2)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.024
CHEMBL411514 160341 0 None 15 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 361 4 0 3 3.7 COC(C#C[C@@]1(OC)CN2CCC1CC2)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.024
118719923 115277 0 None -1 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 621 18 0 7 7.6 CN1CCC=C(c2nsnc2OCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354070 115277 0 None -1 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 621 18 0 7 7.6 CN1CCC=C(c2nsnc2OCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
10193005 76802 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 2 1 4 3.5 C1CCCN(c2nc(C3CC3)nc3c2CCCCN3)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL207816 76802 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 2 1 4 3.5 C1CCCN(c2nc(C3CC3)nc3c2CCCCN3)CC1 10.1016/j.bmcl.2006.01.006
44409944 76971 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2(C)CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL208335 76971 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2(C)CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44311771 163680 0 None -34 3 Human 8.0 pKi = 8 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 546 9 0 6 4.5 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(S(=O)(=O)CCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
CHEMBL421113 163680 0 None -34 3 Human 8.0 pKi = 8 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 546 9 0 6 4.5 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(S(=O)(=O)CCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
44455198 97208 0 None -2 10 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2007.11.022
CHEMBL271108 97208 0 None -2 10 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2007.11.022
44455198 97208 0 None -2 10 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1021/acs.jmedchem.8b00041
CHEMBL271108 97208 0 None -2 10 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1021/acs.jmedchem.8b00041
10316726 11923 0 None -40 5 Rat 8.0 pKi = 8.0 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
CHEMBL1183364 11923 0 None -40 5 Rat 8.0 pKi = 8.0 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
CHEMBL292857 11923 0 None -40 5 Rat 8.0 pKi = 8.0 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
15599352 108136 0 None -2 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL320611 108136 0 None -2 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
44308809 202677 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 5 3 3 2.9 NCC1CCC(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL71799 202677 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 5 3 3 2.9 NCC1CCC(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
135398737 944 89 None -10 91 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 944 89 None -10 91 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 944 89 None -10 91 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 944 89 None -10 91 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 944 89 None -10 91 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398745 2869 108 None -27 65 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 2869 108 None -27 65 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 2869 108 None -27 65 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 2869 108 None -27 65 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
44406387 72498 0 None 5 2 Human 7.0 pKi = 7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 3 1 3 3.7 CO[C@]1(C#CC(O)(c2ccc(C)cc2)c2ccc(C)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200209 72498 0 None 5 2 Human 7.0 pKi = 7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 3 1 3 3.7 CO[C@]1(C#CC(O)(c2ccc(C)cc2)c2ccc(C)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406451 72597 0 None 6 2 Human 7.0 pKi = 7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 385 2 1 3 3.8 CO[C@]1(C#CC(O)C2c3ccccc3C=Cc3ccccc32)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200566 72597 0 None 6 2 Human 7.0 pKi = 7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 385 2 1 3 3.8 CO[C@]1(C#CC(O)C2c3ccccc3C=Cc3ccccc32)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
129989 447 41 None -16 9 Human 7.0 pKi = 7 Binding
Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
8584 447 41 None -16 9 Human 7.0 pKi = 7 Binding
Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
CHEMBL43383 447 41 None -16 9 Human 7.0 pKi = 7 Binding
Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
4011 81996 43 None -14 23 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81996 43 None -14 23 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
155566290 176006 0 None -1318 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4582879 176006 0 None -1318 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4597498 176006 0 None -1318 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44409772 76417 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 304 5 1 5 3.0 CCc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
CHEMBL206826 76417 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 304 5 1 5 3.0 CCc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
44409462 139912 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 340 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C(F)(F)F)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL380926 139912 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 340 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C(F)(F)F)CC1 10.1016/j.bmcl.2006.01.006
44409755 165800 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 258 4 1 4 2.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL427390 165800 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 258 4 1 4 2.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCC1 10.1016/j.bmcl.2006.01.006
42853213 103865 4 None 7 2 Human 7.0 pKi = 7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 360 5 0 3 4.6 O=C(c1ccco1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL310016 103865 4 None 7 2 Human 7.0 pKi = 7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 360 5 0 3 4.6 O=C(c1ccco1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
10468535 97677 1 None -1 3 Human 7.0 pKi = 7 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 273 0 0 1 4.2 c1ccc2c(c1)C(=C1CN3CCC1CC3)c1ccccc1-2 10.1016/S0960-894X(01)80824-6
CHEMBL273586 97677 1 None -1 3 Human 7.0 pKi = 7 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 273 0 0 1 4.2 c1ccc2c(c1)C(=C1CN3CCC1CC3)c1ccccc1-2 10.1016/S0960-894X(01)80824-6
10572657 40298 0 None 4 3 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2cccnc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL148328 40298 0 None 4 3 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2cccnc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
10160219 4861 0 None -100 5 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 436 5 1 5 5.5 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL104693 4861 0 None -100 5 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 436 5 1 5 5.5 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
44406424 72325 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 483 3 1 3 5.1 CO[C@]1(C#CC(O)(c2cccc(C(F)(F)F)c2)c2cccc(C(F)(F)F)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL199591 72325 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 483 3 1 3 5.1 CO[C@]1(C#CC(O)(c2cccc(C(F)(F)F)c2)c2cccc(C(F)(F)F)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
127041952 137473 0 None -39 5 Human 6.0 pKi = 6 Binding
Binding affinity to muscarinic M3 receptor (unknown origin)Binding affinity to muscarinic M3 receptor (unknown origin)
ChEMBL 467 7 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CCOC(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2015.12.081
CHEMBL3764557 137473 0 None -39 5 Human 6.0 pKi = 6 Binding
Binding affinity to muscarinic M3 receptor (unknown origin)Binding affinity to muscarinic M3 receptor (unknown origin)
ChEMBL 467 7 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CCOC(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2015.12.081
3013847 188328 1 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 741 23 5 10 5.8 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
CHEMBL507760 188328 1 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 741 23 5 10 5.8 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
10742178 204354 0 None - 1 Human 6.0 pKi = 6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 449 5 0 3 5.2 O=C(c1ccc(Br)cc1)N(c1cccnc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85511 204354 0 None - 1 Human 6.0 pKi = 6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 449 5 0 3 5.2 O=C(c1ccc(Br)cc1)N(c1cccnc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
44274441 98636 0 None -1 5 Human 5.0 pKi = 5 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL280684 98636 0 None -1 5 Human 5.0 pKi = 5 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
155552923 175733 0 None -213 5 Human 5.0 pKi = 5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4544820 175733 0 None -213 5 Human 5.0 pKi = 5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595245 175733 0 None -213 5 Human 5.0 pKi = 5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
45786849 157263 28 None -1 3 Human 5.0 pKi = 5 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 3 1 3 1.4 c1cncc(COC2CCCNC2)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4083241 157263 28 None -1 3 Human 5.0 pKi = 5 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 3 1 3 1.4 c1cncc(COC2CCCNC2)c1 10.1021/acs.jmedchem.7b01113
56593934 65364 0 None -2630 8 Human 5.0 pKi = 5 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
CHEMBL1834350 65364 0 None -2630 8 Human 5.0 pKi = 5 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
1212 1632 45 None -407 65 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1632 45 None -407 65 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1632 45 None -407 65 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1632 45 None -407 65 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1632 45 None -407 65 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
16125444 167863 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 4 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(c2ccccc2)CC1 10.1021/jm061159a
CHEMBL434929 167863 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 4 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(c2ccccc2)CC1 10.1021/jm061159a
9998202 68824 0 None 2 2 Rat 7.0 pKi = 7.0 Binding
Ki value for rat Muscarinic acetylcholine receptor M3Ki value for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL192485 68824 0 None 2 2 Rat 7.0 pKi = 7.0 Binding
Ki value for rat Muscarinic acetylcholine receptor M3Ki value for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
155562295 174578 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 396 6 0 5 3.9 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4570052 174578 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 396 6 0 5 3.9 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
11015312 5202 0 None -15 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 5 1 5 4.9 CCCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106505 5202 0 None -15 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 5 1 5 4.9 CCCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
324 1894 12 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
6436265 1894 12 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
CHEMBL277642 1894 12 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
145960827 160833 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4126290 160833 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
2551 782 23 None -54 11 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
11024241 119795 0 None -1 5 Human 6.0 pKi = 6.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 338 6 0 3 4.9 CSc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
CHEMBL352723 119795 0 None -1 5 Human 6.0 pKi = 6.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 338 6 0 3 4.9 CSc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
164618698 187948 0 None -11220 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 23 10 13 -0.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4862098 187948 0 None -11220 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 23 10 13 -0.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028512 187948 0 None -11220 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 23 10 13 -0.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
46227485 14008 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198034 14008 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL593620 14008 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
16125565 84336 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 401 5 2 3 3.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2c[nH]cn2)CC1 10.1021/jm061159a
CHEMBL223022 84336 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 401 5 2 3 3.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2c[nH]cn2)CC1 10.1021/jm061159a
73350931 92102 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 279 3 0 2 2.4 CN(Cc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432040 92102 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 279 3 0 2 2.4 CN(Cc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
109035013 179893 1 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 314 4 1 2 4.1 O=C(CCN1CCCc2ccccc21)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2020.127632
CHEMBL4752973 179893 1 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 314 4 1 2 4.1 O=C(CCN1CCCc2ccccc21)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2020.127632
15050952 201802 0 None -1 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 507 9 3 7 1.0 CC(=O)NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL66177 201802 0 None -1 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 507 9 3 7 1.0 CC(=O)NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
73350398 89368 0 None 10 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 363 8 0 4 5.0 CCN(CC)CCOC(=O)c1ccccc1Sc1ccc(Cl)cc1 10.1016/j.bmc.2013.01.072
CHEMBL2377262 89368 0 None 10 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 363 8 0 4 5.0 CCN(CC)CCOC(=O)c1ccccc1Sc1ccc(Cl)cc1 10.1016/j.bmc.2013.01.072
155566290 176006 0 None -1318 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4582879 176006 0 None -1318 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597498 176006 0 None -1318 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
11766733 155213 0 None -549 5 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1121 29 4 10 12.0 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL1202003 155213 0 None -549 5 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1121 29 4 10 12.0 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL405739 155213 0 None -549 5 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1121 29 4 10 12.0 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
49783415 17496 0 None -1479 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 17496 0 None -1479 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
154734599 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
327 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
4108 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
CHEMBL27673 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
156013536 177736 0 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4639297 177736 0 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651058 177736 0 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
154734599 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
327 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
4108 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
CHEMBL27673 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
154734599 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00046a021
327 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00046a021
4108 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00046a021
CHEMBL27673 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00046a021
44299599 167242 0 None -9 4 Human 5.0 pKi = 5.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL430587 167242 0 None -9 4 Human 5.0 pKi = 5.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
54816802 180690 2 None -26 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 2 0 2 2.5 O=C(CN1CCCc2ccccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4762056 180690 2 None -26 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 2 0 2 2.5 O=C(CN1CCCc2ccccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
46227413 14025 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 C[C@@H]1OC[C@@H](C[N+](C)(C)C)O[C@H]1C 10.1016/j.bmc.2009.10.027
CHEMBL1198087 14025 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 C[C@@H]1OC[C@@H](C[N+](C)(C)C)O[C@H]1C 10.1016/j.bmc.2009.10.027
CHEMBL595265 14025 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 C[C@@H]1OC[C@@H](C[N+](C)(C)C)O[C@H]1C 10.1016/j.bmc.2009.10.027
44309153 201820 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 4 2 3 2.5 NCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL66322 201820 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 4 2 3 2.5 NCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
9905731 167943 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 334 6 1 5 2.2 CN(C)C1(CNCCC2CCOCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL435353 167943 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 334 6 1 5 2.2 CN(C)C1(CNCCC2CCOCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
156014558 176650 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 344 4 2 3 4.6 O=C(Nc1ccccc1-c1ccc(Cl)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4635566 176650 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 344 4 2 3 4.6 O=C(Nc1ccccc1-c1ccc(Cl)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
10716120 38048 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 402 7 2 3 3.9 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@@H](F)C2)CC1 10.1021/jm0003135
CHEMBL146249 38048 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 402 7 2 3 3.9 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@@H](F)C2)CC1 10.1021/jm0003135
10573458 118757 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 407 6 2 4 3.5 Cc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)n1 10.1021/jm0003135
CHEMBL343659 118757 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 407 6 2 4 3.5 Cc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)n1 10.1021/jm0003135
44337760 9175 0 None -2 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 335 4 0 3 3.8 CN1CC2CC1C[C@H](OC(=O)C(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL110808 9175 0 None -2 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 335 4 0 3 3.8 CN1CC2CC1C[C@H](OC(=O)C(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
73353378 89372 0 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 331 4 1 4 2.4 CN1CCC(OC(=O)C(CO)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2013.01.072
CHEMBL2377268 89372 0 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 331 4 1 4 2.4 CN1CCC(OC(=O)C(CO)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2013.01.072
137628800 160447 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 248 4 0 1 2.8 C[N+](C)(C)CCc1cccc(OC(F)(F)F)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4089027 160447 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 248 4 0 1 2.8 C[N+](C)(C)CCc1cccc(OC(F)(F)F)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116151 160447 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 248 4 0 1 2.8 C[N+](C)(C)CCc1cccc(OC(F)(F)F)c1 10.1021/acs.jmedchem.7b01113
3055 1405 43 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
313 1405 43 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
7163 1405 43 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
CHEMBL936 1405 43 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
DB01231 1405 43 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
44337638 110077 0 None -1 2 Rat 5.0 pKi = 5.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL325322 110077 0 None -1 2 Rat 5.0 pKi = 5.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
16125508 83915 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 412 5 1 3 4.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccnc2)CC1 10.1021/jm061159a
CHEMBL221660 83915 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 412 5 1 3 4.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccnc2)CC1 10.1021/jm061159a
16125224 136227 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 471 7 1 4 4.6 COc1ccc(C2(c3ccc(OC)cc3)CN(C3CCN(Cc4ccccc4)CC3)C(=O)N2)cc1 10.1021/jm061159a
CHEMBL374099 136227 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 471 7 1 4 4.6 COc1ccc(C2(c3ccc(OC)cc3)CN(C3CCN(Cc4ccccc4)CC3)C(=O)N2)cc1 10.1021/jm061159a
10771937 21493 0 None -204 5 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL1202004 21493 0 None -204 5 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL131846 21493 0 None -204 5 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
44318851 104247 0 None -60 4 Human 4.9 pKi = 4.9 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL310558 104247 0 None -60 4 Human 4.9 pKi = 4.9 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
164613559 187902 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 874 21 9 12 0.2 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4856659 187902 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 874 21 9 12 0.2 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028196 187902 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 874 21 9 12 0.2 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
155557119 175937 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4555411 175937 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596899 175937 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
162353379 180380 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 3 0 2 2.1 O=C(CCN1CCCc2ccccc21)N1CCC1 10.1016/j.bmcl.2020.127632
CHEMBL4758449 180380 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 3 0 2 2.1 O=C(CCN1CCCc2ccccc21)N1CCC1 10.1016/j.bmcl.2020.127632
3675988 176261 63 None 1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc(C2CCCN2)c1 10.1021/jm800145d
CHEMBL461087 176261 63 None 1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc(C2CCCN2)c1 10.1021/jm800145d
155516095 169489 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 366 5 0 4 3.9 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4442996 169489 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 366 5 0 4 3.9 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
542182 101691 1 None -1 3 Rat 4.9 pKi = 4.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 465 8 3 7 0.8 NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL302604 101691 1 None -1 3 Rat 4.9 pKi = 4.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 465 8 3 7 0.8 NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
16125505 84354 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 6 1 2 4.7 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCc2ccccc2)CC1 10.1021/jm061159a
CHEMBL223186 84354 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 6 1 2 4.7 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCc2ccccc2)CC1 10.1021/jm061159a
11012712 57524 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
CHEMBL167027 57524 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
11000399 58786 0 None -2 5 Human 4.9 pKi = 4.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccncc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL169680 58786 0 None -2 5 Human 4.9 pKi = 4.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccncc2)c2ccccc2C1 10.1021/jm020895l
118719925 115279 0 None -158 8 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/jm501173q
CHEMBL3354072 115279 0 None -158 8 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/jm501173q
44400185 68984 0 None 1 2 Rat 6.9 pKi = 6.9 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@@]3(C)C2)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
CHEMBL192885 68984 0 None 1 2 Rat 6.9 pKi = 6.9 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@@]3(C)C2)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
59291324 112281 0 None -1 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1scnc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298593 112281 0 None -1 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1scnc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305622 112281 0 None -1 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1scnc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
10835518 40086 0 None 16 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 412 6 2 3 4.6 O=C(NC1CCN(CC2CCCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL148129 40086 0 None 16 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 412 6 2 3 4.6 O=C(NC1CCN(CC2CCCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
44443735 93947 0 None 52 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 448 7 2 5 3.1 O=C(N[C@H]1[C@@H]2CN(CCc3ccc4c(c3)OCO4)C[C@@H]21)[C@](O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL250834 93947 0 None 52 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 448 7 2 5 3.1 O=C(N[C@H]1[C@@H]2CN(CCc3ccc4c(c3)OCO4)C[C@@H]21)[C@](O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
44443733 154246 0 None 45 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)[C@](O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL400167 154246 0 None 45 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)[C@](O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
44337747 109185 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 425 6 0 3 5.6 CC(C(=O)O[C@H]1CC2CC(C1)N(Cc1ccccc1)C2)(c1ccccc1)c1ccccc1 10.1021/jm00115a003
CHEMBL322582 109185 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 425 6 0 3 5.6 CC(C(=O)O[C@H]1CC2CC(C1)N(Cc1ccccc1)C2)(c1ccccc1)c1ccccc1 10.1021/jm00115a003
CHEMBL5076535 212674 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44308831 202690 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 6 2 3 3.2 CNCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL71933 202690 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 6 2 3 3.2 CNCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
15050955 102125 0 None -1 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 538 7 1 7 3.0 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCCN3C(=O)c4ccccc4C3=O)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL304112 102125 0 None -1 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 538 7 1 7 3.0 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCCN3C(=O)c4ccccc4C3=O)CC2)c2ccccc21 10.1021/jm00111a032
24936155 94185 0 None -199 7 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 10.1016/j.bmcl.2007.10.109
CHEMBL252258 94185 0 None -199 7 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 10.1016/j.bmcl.2007.10.109
137630127 160502 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 210 4 1 2 1.4 COc1cccc(C(O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4084607 160502 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 210 4 1 2 1.4 COc1cccc(C(O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116537 160502 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 210 4 1 2 1.4 COc1cccc(C(O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
137630848 160569 0 None -1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 213 3 0 3 1.5 C[N+]1(C)CCC(OCc2nccs2)C1 10.1021/acs.jmedchem.7b01113
CHEMBL4061390 160569 0 None -1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 213 3 0 3 1.5 C[N+]1(C)CCC(OCc2nccs2)C1 10.1021/acs.jmedchem.7b01113
CHEMBL4117131 160569 0 None -1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 213 3 0 3 1.5 C[N+]1(C)CCC(OCc2nccs2)C1 10.1021/acs.jmedchem.7b01113
71452790 79240 0 None 1 2 Rat 4.9 pKi = 4.9 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)O[C@H]1CC2CC1CN2C 10.1021/jm00090a006
CHEMBL2115122 79240 0 None 1 2 Rat 4.9 pKi = 4.9 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)O[C@H]1CC2CC1CN2C 10.1021/jm00090a006
164619973 187956 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4862996 187956 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028571 187956 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
10236758 115272 3 None -1230 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 115272 3 None -1230 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
109018479 181236 1 None -9 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 5 1 3 2.7 O=C(CCN1CCCc2ccccc21)NCc1ccco1 10.1016/j.bmcl.2020.127632
CHEMBL4778178 181236 1 None -9 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 5 1 3 2.7 O=C(CCN1CCCc2ccccc21)NCc1ccco1 10.1016/j.bmcl.2020.127632
7141656 176263 6 None -3 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc([C@H]2CCCN2)o1 10.1021/jm800145d
CHEMBL461089 176263 6 None -3 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc([C@H]2CCCN2)o1 10.1021/jm800145d
44311760 202794 0 None -316 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 510 8 0 5 5.0 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(C(=O)CCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
CHEMBL72551 202794 0 None -316 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 510 8 0 5 5.0 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(C(=O)CCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
71463063 83387 0 None -1 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205825 83387 0 None -1 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
44448419 12230 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 580 16 2 2 7.0 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CCC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185266 12230 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 580 16 2 2 7.0 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CCC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL403592 12230 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 580 16 2 2 7.0 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CCC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
10226457 12866 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL1189471 12866 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL538793 12866 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
3013845 188163 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 729 21 5 11 5.1 CCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL505197 188163 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 729 21 5 11 5.1 CCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
155557119 175937 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4555411 175937 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4596899 175937 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
155548586 176023 0 None -234 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 562 12 6 6 2.5 N=C(N)NCCC[C@H](N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4537517 176023 0 None -234 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 562 12 6 6 2.5 N=C(N)NCCC[C@H](N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597611 176023 0 None -234 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 562 12 6 6 2.5 N=C(N)NCCC[C@H](N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
44409977 75701 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 6 2 5 3.9 Cc1c(NCc2cccs2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL205737 75701 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 6 2 5 3.9 Cc1c(NCc2cccs2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
44409961 138711 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 1 4 3.7 Cc1c(NC2CC2)nc(CC2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL378904 138711 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 1 4 3.7 Cc1c(NC2CC2)nc(CC2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
2551 782 23 None -54 11 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
162677513 183162 0 None -39 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 983 17 3 11 6.2 CN(C)c1ccc2c(-c3ccc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
CHEMBL4789147 183162 0 None -39 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 983 17 3 11 6.2 CN(C)c1ccc2c(-c3ccc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
CHEMBL4803695 183162 0 None -39 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 983 17 3 11 6.2 CN(C)c1ccc2c(-c3ccc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
155540315 172344 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 398 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CCN(C)CC2)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4516350 172344 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 398 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CCN(C)CC2)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL1200633 206858 3 None -4 8 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(CC[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(CC[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
162353393 178859 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 312 5 1 2 3.3 O=C(CCN1CCCc2ccccc21)NCc1cccc(F)c1 10.1016/j.bmcl.2020.127632
CHEMBL4740422 178859 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 312 5 1 2 3.3 O=C(CCN1CCCc2ccccc21)NCc1cccc(F)c1 10.1016/j.bmcl.2020.127632
44406520 134735 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 CO[C@]1(C#C[C@](O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL372566 134735 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 CO[C@]1(C#C[C@](O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
3652 4034 72 None -3 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 4034 72 None -3 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 4034 72 None -3 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 4034 72 None -3 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 4034 72 None -3 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
44430473 143119 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.2 CC1CN(c2cc(N3CCCCCC3)nc(C3CC3)n2)C1 10.1016/j.bmcl.2007.03.047
CHEMBL389992 143119 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.2 CC1CN(c2cc(N3CCCCCC3)nc(C3CC3)n2)C1 10.1016/j.bmcl.2007.03.047
44409558 75574 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 4 1 4 3.2 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205105 75574 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 4 1 4 3.2 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCC1 10.1016/j.bmcl.2006.01.006
10836338 39096 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 429 6 2 4 3.5 O=C(NC1CCN(Cc2ccccn2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL147105 39096 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 429 6 2 4 3.5 O=C(NC1CCN(Cc2ccccn2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
155525097 170383 0 None -165 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 712 13 1 10 5.5 CN1CC=C(c2nsnc2OCCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4455570 170383 0 None -165 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 712 13 1 10 5.5 CN1CC=C(c2nsnc2OCCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)CC1 10.1021/acs.jmedchem.8b01967
154059 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
2457 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
7483 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
CHEMBL1734 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
DB01591 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
16125223 168333 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 5 1 2 4.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm061159a
CHEMBL438427 168333 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 5 1 2 4.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm061159a
16125509 168776 0 None 69 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 3 4.7 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccs2)CC1 10.1021/jm061159a
CHEMBL441873 168776 0 None 69 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 3 4.7 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccs2)CC1 10.1021/jm061159a
155523648 176019 0 None -91 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 909 18 6 9 5.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4454300 176019 0 None -91 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 909 18 6 9 5.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597576 176019 0 None -91 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 909 18 6 9 5.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
10225340 202631 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 441 6 0 5 4.8 COc1ccc(S(=O)(=O)c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL71531 202631 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 441 6 0 5 4.8 COc1ccc(S(=O)(=O)c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
16125566 141000 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2Cl)CC1 10.1021/jm061159a
CHEMBL384670 141000 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2Cl)CC1 10.1021/jm061159a
155551306 173389 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 396 6 0 3 4.8 Cc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
CHEMBL4541518 173389 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 396 6 0 3 4.8 Cc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
3013846 187656 2 None 1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL499519 187656 2 None 1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
11567493 200117 9 None -5 3 Rat 5.9 pKi = 5.9 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1 10.1021/jm050099q
CHEMBL606902 200117 9 None -5 3 Rat 5.9 pKi = 5.9 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1 10.1021/jm050099q
10105296 204206 0 None -4 4 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
CHEMBL84113 204206 0 None -4 4 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
10386 160621 13 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 180 3 1 1 1.6 C[N+](C)(C)CCc1cccc(O)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4092348 160621 13 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 180 3 1 1 1.6 C[N+](C)(C)CCc1cccc(O)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4117554 160621 13 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 180 3 1 1 1.6 C[N+](C)(C)CCc1cccc(O)c1 10.1021/acs.jmedchem.7b01113
73346336 92113 0 None -2 6 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 2 3.0 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432054 92113 0 None -2 6 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 2 3.0 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
71449073 78172 0 None -3 4 Rat 5.9 pKi = 5.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 338 2 2 6 0.6 O=C1Nc2cccnc2N(C(=O)CN2CCNCC2)c2ncccc21 10.1021/jm00111a032
CHEMBL2112217 78172 0 None -3 4 Rat 5.9 pKi = 5.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 338 2 2 6 0.6 O=C1Nc2cccnc2N(C(=O)CN2CCNCC2)c2ncccc21 10.1021/jm00111a032
164610746 187883 0 None -3388 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4854886 187883 0 None -3388 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028038 187883 0 None -3388 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156015051 177753 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4643329 177753 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651139 177753 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
156009660 177754 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4634475 177754 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4651150 177754 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
155549890 173336 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CCCN(C)C2)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4540291 173336 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CCCN(C)C2)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
135423423 188419 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 813 27 5 11 7.5 CCCCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL508807 188419 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 813 27 5 11 7.5 CCCCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
156010212 177662 0 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4634066 177662 0 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650562 177662 0 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
137645938 157041 0 None -977 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4080675 157041 0 None -977 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
657347 5007 2 None -114 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.5 C[C@H]1OC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
CHEMBL105457 5007 2 None -114 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.5 C[C@H]1OC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
CHEMBL387632 5007 2 None -114 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.5 C[C@H]1OC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
107782 14330 16 None -1 5 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
67151996 14330 16 None -1 5 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
CHEMBL1201207 14330 16 None -1 5 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
1224 1404 79 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1404 79 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1404 79 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1404 79 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1404 79 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1404 79 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3191 102385 93 None -6 25 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102385 93 None -6 25 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
10595006 11340 0 None -8 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL1180343 11340 0 None -8 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL123099 11340 0 None -8 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
10104 3510 7 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
6604866 3510 7 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
CHEMBL1493369 3510 7 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
155525065 175980 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 590 11 4 6 2.9 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4456524 175980 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 590 11 4 6 2.9 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597243 175980 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 590 11 4 6 2.9 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
10874119 4838 0 None -19 5 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 454 4 1 5 5.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OCc5ccccc5)c34)OC21 10.1021/jm011116o
CHEMBL104574 4838 0 None -19 5 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 454 4 1 5 5.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OCc5ccccc5)c34)OC21 10.1021/jm011116o
2551 782 23 None -54 11 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
53324553 56560 0 None -1 10 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL1643900 56560 0 None -1 10 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
53324553 56560 0 None -1 10 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
CHEMBL1643900 56560 0 None -1 10 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
44400323 68327 0 None 2 2 Rat 7.9 pKi = 7.9 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 361 5 1 4 2.4 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.02.036
CHEMBL192065 68327 0 None 2 2 Rat 7.9 pKi = 7.9 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 361 5 1 4 2.4 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.02.036
44431386 148493 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 332 5 1 5 2.1 CN(C)C1(CNCC=C2CCOCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL394255 148493 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 332 5 1 5 2.1 CN(C)C1(CNCC=C2CCOCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
53321085 58208 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 366 7 1 3 5.6 CCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683913 58208 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 366 7 1 3 5.6 CCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
138710710 176471 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1ccc(Cl)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4632545 176471 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1ccc(Cl)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
11794901 119078 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2ccccn2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL346194 119078 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2ccccn2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
53372934 128778 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670826 128778 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
156015390 177667 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4648229 177667 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650585 177667 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
53319789 58236 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 667 16 5 6 7.1 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1C[N+]2(CCCCCCCCCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)CCC1CC2 10.1016/j.bmcl.2011.01.043
CHEMBL1683941 58236 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 667 16 5 6 7.1 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1C[N+]2(CCCCCCCCCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)CCC1CC2 10.1016/j.bmcl.2011.01.043
137629887 160463 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 218 4 0 1 3.1 C[N+](C)(C)CCCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4065555 160463 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 218 4 0 1 3.1 C[N+](C)(C)CCCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116259 160463 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 218 4 0 1 3.1 C[N+](C)(C)CCCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
155535972 171556 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 356 5 0 3 4.1 CN1CCC(OC(=O)N(CCc2ccc(F)cc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.12.022
CHEMBL4472832 171556 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 356 5 0 3 4.1 CN1CCC(OC(=O)N(CCc2ccc(F)cc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.12.022
71720488 86525 0 None -2 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 337 3 0 5 2.7 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3Cl)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323441 86525 0 None -2 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 337 3 0 5 2.7 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3Cl)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
137628799 160446 0 None -14 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 212 4 0 1 2.1 COc1ccc(F)c(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4064668 160446 0 None -14 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 212 4 0 1 2.1 COc1ccc(F)c(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116150 160446 0 None -14 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 212 4 0 1 2.1 COc1ccc(F)c(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
1836 2554 56 None -42 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 2554 56 None -42 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 2554 56 None -42 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 2554 56 None -42 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 2554 56 None -42 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
44337638 110077 0 None -1 2 Rat 4.9 pKi = 4.9 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL325322 110077 0 None -1 2 Rat 4.9 pKi = 4.9 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
44274302 76714 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL20732 76714 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
137640511 156524 0 None -54 8 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4074104 156524 0 None -54 8 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
156014450 177676 0 None -794 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 518 9 2 6 3.4 NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4636083 177676 0 None -794 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 518 9 2 6 3.4 NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4650652 177676 0 None -794 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 518 9 2 6 3.4 NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
145961152 161043 0 None -8 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4129382 161043 0 None -8 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
44437259 11774 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 297 4 0 3 3.0 C[N+]1(CC#CCOc2cc(-c3ccccc3)on2)CCCC1 10.1016/j.bmc.2007.09.003
CHEMBL1182448 11774 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 297 4 0 3 3.0 C[N+]1(CC#CCOc2cc(-c3ccccc3)on2)CCCC1 10.1016/j.bmc.2007.09.003
CHEMBL239038 11774 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 297 4 0 3 3.0 C[N+]1(CC#CCOc2cc(-c3ccccc3)on2)CCCC1 10.1016/j.bmc.2007.09.003
156014820 177730 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4646116 177730 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4650998 177730 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
132947 3803 8 None -309 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/j.bmc.2008.06.025
361 3803 8 None -309 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/j.bmc.2008.06.025
CHEMBL265256 3803 8 None -309 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/j.bmc.2008.06.025
156014820 177730 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
CHEMBL4646116 177730 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
CHEMBL4650998 177730 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
132947 3803 8 None -999 9 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm981038d
361 3803 8 None -999 9 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm981038d
CHEMBL265256 3803 8 None -999 9 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm981038d
155521383 175852 0 None -131 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 604 13 6 6 2.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4450522 175852 0 None -131 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 604 13 6 6 2.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596184 175852 0 None -131 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 604 13 6 6 2.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
46878250 200174 0 None -1 2 Rat 4.8 pKi = 4.8 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@H]1CC2CC(C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL607175 200174 0 None -1 2 Rat 4.8 pKi = 4.8 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@H]1CC2CC(C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
3158 55974 21 None -104 20 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55974 21 None -104 20 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
10670961 40391 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 5 3.1 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)nc1 10.1021/jm0003135
CHEMBL148404 40391 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 5 3.1 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)nc1 10.1021/jm0003135
137630050 160493 0 None -42 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
CHEMBL4089543 160493 0 None -42 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
CHEMBL4097258 160493 0 None -42 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
CHEMBL4116470 160493 0 None -42 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
10171655 86578 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.3 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
CHEMBL232419 86578 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.3 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
10269809 158834 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 345 3 0 2 4.1 COC1(C#CC(C)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL410061 158834 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 345 3 0 2 4.1 COC1(C#CC(C)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
44319010 204112 0 None 15 2 Human 7.8 pKi = 7.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 348 5 0 2 4.5 O=C(C1CCC1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL83363 204112 0 None 15 2 Human 7.8 pKi = 7.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 348 5 0 2 4.5 O=C(C1CCC1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
46878242 200126 0 None -13 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1C[C@H](O)c2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
CHEMBL606962 200126 0 None -13 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1C[C@H](O)c2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
16086015 12195 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 1 4 4.6 NCC1CCN(C(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)CC1 10.1021/jm051205r
CHEMBL1184933 12195 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 1 4 4.6 NCC1CCN(C(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)CC1 10.1021/jm051205r
CHEMBL379055 12195 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 1 4 4.6 NCC1CCN(C(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)CC1 10.1021/jm051205r
CHEMBL306462 102492 0 None -1 5 Human 5.8 pKi = 5.8 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 211 2 1 4 1.1 CCO/C(O)=C1\CN2CCCC(C2)C1=O 10.1021/jm020572p
44328540 206047 0 None -4 3 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 245 3 1 3 2.3 COc1ccccc1C(O)C1=CN2CCC1CC2 10.1016/S0960-894X(01)80824-6
CHEMBL96042 206047 0 None -4 3 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 245 3 1 3 2.3 COc1ccccc1C(O)C1=CN2CCC1CC2 10.1016/S0960-894X(01)80824-6
10035281 100513 0 None -6 8 Human 4.8 pKi = 4.8 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL294273 100513 0 None -6 8 Human 4.8 pKi = 4.8 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
10035281 100513 0 None -6 8 Rat 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
CHEMBL294273 100513 0 None -6 8 Rat 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
10035281 100513 0 None -6 8 Human 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
CHEMBL294273 100513 0 None -6 8 Human 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
10160073 110701 0 None -151 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm301774u
CHEMBL326450 110701 0 None -151 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm301774u
155543944 175760 0 None -426 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 873 21 6 10 2.3 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4567026 175760 0 None -426 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 873 21 6 10 2.3 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595467 175760 0 None -426 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 873 21 6 10 2.3 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
10160073 110701 0 None -151 5 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL326450 110701 0 None -151 5 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
639794 98314 1 None -1 5 Human 4.8 pKi = 4.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL278129 98314 1 None -1 5 Human 4.8 pKi = 4.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
19021478 192096 0 None -11 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to Muscarinic acetylcholine receptor M3 (unknown origin) assessed as inhibition constantBinding affinity to Muscarinic acetylcholine receptor M3 (unknown origin) assessed as inhibition constant
ChEMBL 356 4 1 3 4.5 CNC(=O)Oc1cccc2c1CCC1C2CCN1CCC1CCCCC1 10.1016/j.ejmech.2022.114606
CHEMBL5219452 192096 0 None -11 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to Muscarinic acetylcholine receptor M3 (unknown origin) assessed as inhibition constantBinding affinity to Muscarinic acetylcholine receptor M3 (unknown origin) assessed as inhibition constant
ChEMBL 356 4 1 3 4.5 CNC(=O)Oc1cccc2c1CCC1C2CCN1CCC1CCCCC1 10.1016/j.ejmech.2022.114606
16125437 83930 0 None 19 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 439 7 1 2 4.9 O=C1NC(Cc2ccccc2)(Cc2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL221713 83930 0 None 19 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 439 7 1 2 4.9 O=C1NC(Cc2ccccc2)(Cc2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
44420791 84280 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 376 3 1 1 3.7 C[N+]1(C)C2CCC1CC(N1CC(c3ccccc3)(c3ccccc3)NC1=O)C2 10.1021/jm061160+
CHEMBL222689 84280 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 376 3 1 1 3.7 C[N+]1(C)C2CCC1CC(N1CC(c3ccccc3)(c3ccccc3)NC1=O)C2 10.1021/jm061160+
155554568 176035 0 None -363 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 702 14 4 8 2.6 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4548432 176035 0 None -363 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 702 14 4 8 2.6 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597724 176035 0 None -363 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 702 14 4 8 2.6 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
156016041 177672 0 None -38 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1238 28 4 13 9.9 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCNC(=O)CCc3cn(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)cn3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4644612 177672 0 None -38 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1238 28 4 13 9.9 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCNC(=O)CCc3cn(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)cn3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650627 177672 0 None -38 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1238 28 4 13 9.9 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCNC(=O)CCc3cn(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)cn3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
44627956 13920 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197362 13920 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL568775 13920 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
101676031 96879 0 None -32 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
16175987 96879 0 None -32 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL1201998 96879 0 None -32 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL269272 96879 0 None -32 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
122194376 123373 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 366 7 1 3 3.4 COc1ccc(CCC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3627739 123373 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 366 7 1 3 3.4 COc1ccc(CCC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
10880435 58750 0 None -6 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL169494 58750 0 None -6 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
156015719 177683 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4646457 177683 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650699 177683 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
145961981 160984 0 None -7 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4128497 160984 0 None -7 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
11729182 5160 0 None -3 5 Human 4.8 pKi = 4.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 405 3 1 4 4.0 CCN(C)C(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106259 5160 0 None -3 5 Human 4.8 pKi = 4.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 405 3 1 4 4.0 CCN(C)C(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
155521639 170127 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 424 8 0 5 4.4 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4451822 170127 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 424 8 0 5 4.4 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
2200 3082 38 None -15 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
328 3082 38 None -15 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
4848 3082 38 None -15 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
CHEMBL9967 3082 38 None -15 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
DB00670 3082 38 None -15 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
44430462 91874 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 302 3 1 5 2.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(O)C1 10.1016/j.bmcl.2007.03.047
CHEMBL242822 91874 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 302 3 1 5 2.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(O)C1 10.1016/j.bmcl.2007.03.047
44409654 75177 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 326 4 1 4 4.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC2(CCCC2)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL204353 75177 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 326 4 1 4 4.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC2(CCCC2)CC1 10.1016/j.bmcl.2006.01.006
129989 447 41 None -48 9 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
8584 447 41 None -48 9 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
CHEMBL43383 447 41 None -48 9 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
44430467 151557 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 304 3 0 4 3.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(F)C1 10.1016/j.bmcl.2007.03.047
CHEMBL396761 151557 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 304 3 0 4 3.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(F)C1 10.1016/j.bmcl.2007.03.047
44319008 204048 0 None 2 2 Human 6.8 pKi = 6.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 386 4 0 2 4.5 CC(=O)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL82850 204048 0 None 2 2 Human 6.8 pKi = 6.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 386 4 0 2 4.5 CC(=O)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
44318969 204360 0 None 3 2 Human 6.8 pKi = 6.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 384 6 0 2 5.0 O=C(c1ccccc1)N(Cc1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85568 204360 0 None 3 2 Human 6.8 pKi = 6.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 384 6 0 2 5.0 O=C(c1ccccc1)N(Cc1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
10651844 114990 0 None -16 5 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 649 22 3 7 5.2 CN(CCCCCCCCN(C)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
CHEMBL335115 114990 0 None -16 5 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 649 22 3 7 5.2 CN(CCCCCCCCN(C)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
155554262 175981 0 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 797 15 6 7 5.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4582069 175981 0 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 797 15 6 7 5.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597244 175981 0 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 797 15 6 7 5.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
16094788 141383 0 None -125 5 Human 5.8 pKi = 5.8 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL386983 141383 0 None -125 5 Human 5.8 pKi = 5.8 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
6726 1254 46 None -6 13 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1254 46 None -6 13 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1254 46 None -6 13 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1254 46 None -6 13 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1254 46 None -6 13 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
44308913 202269 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 381 4 2 4 0.9 NCC(=O)N1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL69402 202269 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 381 4 2 4 0.9 NCC(=O)N1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
5282593 54972 25 None -1 5 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
CHEMBL1319362 54972 25 None -1 5 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
CHEMBL1618018 54972 25 None -1 5 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
10171655 86578 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.3 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
CHEMBL232419 86578 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.3 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
44409759 75681 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205686 75681 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCCC1 10.1016/j.bmcl.2006.01.006
10236397 76959 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL208280 76959 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C)CC1 10.1016/j.bmcl.2006.01.006
11796409 38155 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 420 7 2 3 4.2 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CCC(F)(F)C2)CC1 10.1021/jm0003135
CHEMBL146351 38155 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 420 7 2 3 4.2 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CCC(F)(F)C2)CC1 10.1021/jm0003135
155521894 175851 0 None -204 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4451383 175851 0 None -204 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596183 175851 0 None -204 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
16125568 96881 0 None 17 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm061159a
CHEMBL269280 96881 0 None 17 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm061159a
16124710 84761 0 None 54 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 412 5 0 3 5.0 O=C1OC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL225387 84761 0 None 54 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 412 5 0 3 5.0 O=C1OC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
156015648 177740 0 None -87 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1021 18 5 12 5.5 NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.9b02172
CHEMBL4641328 177740 0 None -87 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1021 18 5 12 5.5 NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.9b02172
CHEMBL4651078 177740 0 None -87 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1021 18 5 12 5.5 NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.9b02172
15157140 99412 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 359 10 0 3 5.2 CCN(CC)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL285898 99412 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 359 10 0 3 5.2 CCN(CC)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
11718570 71858 0 None -8 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 376 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1Cc1ccccc1 10.1021/jm050099q
CHEMBL198065 71858 0 None -8 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 376 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1Cc1ccccc1 10.1021/jm050099q
11532924 137854 0 None -47 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to muscarinic M3RBinding affinity to muscarinic M3R
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377241 137854 0 None -47 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to muscarinic M3RBinding affinity to muscarinic M3R
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
137628855 160423 0 None -5 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 1 1 1 2.0 C[N+](C)(C)C1CCc2cccc(O)c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL4103087 160423 0 None -5 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 1 1 1 2.0 C[N+](C)(C)C1CCc2cccc(O)c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL4115966 160423 0 None -5 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 1 1 1 2.0 C[N+](C)(C)C1CCc2cccc(O)c2C1 10.1021/acs.jmedchem.7b01113
71452387 83389 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2012.08.046
CHEMBL2205829 83389 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2012.08.046
71452387 83389 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2205829 83389 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmc.2013.07.045
1547484 927 70 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 927 70 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 927 70 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 927 70 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 927 70 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
44593626 187270 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496306 187270 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539121 187270 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
10360219 101540 0 None -16 4 Human 5.8 pKi = 5.8 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL301670 101540 0 None -16 4 Human 5.8 pKi = 5.8 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
155559741 175713 0 None -891 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4562770 175713 0 None -891 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595125 175713 0 None -891 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
145961126 161005 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4128764 161005 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
46227483 14010 0 None 1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198039 14010 0 None 1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL593685 14010 0 None 1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
16125506 84355 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 439 7 1 2 5.1 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCCc2ccccc2)CC1 10.1021/jm061159a
CHEMBL223187 84355 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 439 7 1 2 5.1 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCCc2ccccc2)CC1 10.1021/jm061159a
44275807 98513 0 None -1513 10 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human muscarinic M3 receptorBinding affinity towards human muscarinic M3 receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
CHEMBL27979 98513 0 None -1513 10 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human muscarinic M3 receptorBinding affinity towards human muscarinic M3 receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
44627856 195813 0 None -1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569953 195813 0 None -1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
9998508 79700 0 None -4 5 Human 5.8 pKi = 5.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21321 79700 0 None -4 5 Human 5.8 pKi = 5.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
156015968 177670 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4648657 177670 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650620 177670 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
156015809 177743 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(Sc3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4645019 177743 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(Sc3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651096 177743 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(Sc3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
145962050 161083 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4130037 161083 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
44309089 102536 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 5 3 3 2.4 O=C(NCC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL306903 102536 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 5 3 3 2.4 O=C(NCC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
44309208 165097 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 3 2 3 2.1 O=C(N1CCCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL424416 165097 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 3 2 3 2.1 O=C(N1CCCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
135398737 944 89 None -10 91 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 944 89 None -10 91 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 944 89 None -10 91 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 944 89 None -10 91 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 944 89 None -10 91 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
53321084 58207 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 352 6 1 3 5.2 CCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683912 58207 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 352 6 1 3 5.2 CCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
140844410 175818 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 10 1 3 5.5 O=C(OC1C[N+]2(CCCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4436947 175818 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 10 1 3 5.5 O=C(OC1C[N+]2(CCCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4595946 175818 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 10 1 3 5.5 O=C(OC1C[N+]2(CCCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
10647553 39480 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 458 7 3 4 3.6 O=C(NC1CCN(Cc2cccc(CO)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL147554 39480 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 458 7 3 4 3.6 O=C(NC1CCN(Cc2cccc(CO)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
10739662 42031 0 None 11 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 398 6 2 3 4.2 O=C(NC1CCN(CC2CCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL149769 42031 0 None 11 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 398 6 2 3 4.2 O=C(NC1CCN(CC2CCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
44568347 191055 0 None -8 15 Human 6.8 pKi = 6.8 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL519609 191055 0 None -8 15 Human 6.8 pKi = 6.8 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
16086035 11720 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 NC1CCCC(NC(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)C1 10.1021/jm051205r
CHEMBL1182110 11720 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 NC1CCCC(NC(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)C1 10.1021/jm051205r
CHEMBL212530 11720 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 NC1CCCC(NC(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)C1 10.1021/jm051205r
44328356 110988 0 None - 1 Human 4.8 pKi = 4.8 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 305 1 1 3 3.6 OC1(C2=CN3CCC2CC3)c2ccccc2Oc2ccccc21 10.1016/S0960-894X(01)80824-6
CHEMBL327664 110988 0 None - 1 Human 4.8 pKi = 4.8 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 305 1 1 3 3.6 OC1(C2=CN3CCC2CC3)c2ccccc2Oc2ccccc21 10.1016/S0960-894X(01)80824-6
71459604 83379 0 None -3 14 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83379 0 None -3 14 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
71455894 83388 0 None -1 12 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205827 83388 0 None -1 12 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
71455894 83388 0 None -1 12 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2205827 83388 0 None -1 12 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmc.2013.07.045
2200 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
328 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
4848 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
CHEMBL9967 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
DB00670 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
2200 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
328 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
4848 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
CHEMBL9967 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
DB00670 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
164627445 188022 0 None -812 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 8 11 1.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4876453 188022 0 None -812 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 8 11 1.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028997 188022 0 None -812 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 8 11 1.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
2200 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
328 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
4848 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
CHEMBL9967 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
DB00670 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
2200 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00046a021
328 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00046a021
4848 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00046a021
CHEMBL9967 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00046a021
DB00670 3082 38 None -22 13 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00046a021
14939891 168798 0 None -239 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL442014 168798 0 None -239 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
10043954 81866 0 None -5 5 Human 5.8 pKi = 5.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21716 81866 0 None -5 5 Human 5.8 pKi = 5.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
46682613 180574 1 None -31 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 4 1 2 3.3 O=C(CCN1CCCc2ccccc21)NC1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4760823 180574 1 None -31 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 4 1 2 3.3 O=C(CCN1CCCc2ccccc21)NC1CCCCC1 10.1016/j.bmcl.2020.127632
44448417 11804 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 550 16 2 4 6.7 CN(CCCN(C)CCCC(O)(c1ccccc1)c1ccccc1)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1182629 11804 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 550 16 2 4 6.7 CN(CCCN(C)CCCC(O)(c1ccccc1)c1ccccc1)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL256923 11804 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 550 16 2 4 6.7 CN(CCCN(C)CCCC(O)(c1ccccc1)c1ccccc1)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
11759379 120264 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 332 5 0 2 5.1 CC(C1=C(CCN2CCCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL355392 120264 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 332 5 0 2 5.1 CC(C1=C(CCN2CCCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
57326140 76826 0 None -2 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL2042400 76826 0 None -2 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL2078962 76826 0 None -2 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
14925759 157494 6 None -6165 13 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 157494 6 None -6165 13 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
24894635 169240 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@@H]1c1ccco1 10.1021/jm800145d
CHEMBL443939 169240 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@@H]1c1ccco1 10.1021/jm800145d
CHEMBL527880 169240 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@@H]1c1ccco1 10.1021/jm800145d
15157141 92369 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 373 11 0 3 5.6 CCN(CC)CCCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL24369 92369 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 373 11 0 3 5.6 CCN(CC)CCCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
2247 502 77 None -19 41 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -19 41 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -19 41 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -19 41 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -19 41 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
73346332 92103 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 297 3 0 2 2.6 CN(Cc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432041 92103 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 297 3 0 2 2.6 CN(Cc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
11501540 133080 0 None -3 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1cccs1 10.1021/jm050099q
CHEMBL371293 133080 0 None -3 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1cccs1 10.1021/jm050099q
44431369 87555 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 340 6 1 4 2.9 Cc1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 10.1016/j.bmcl.2006.11.058
CHEMBL234253 87555 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 340 6 1 4 2.9 Cc1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 10.1016/j.bmcl.2006.11.058
90666104 108847 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219034 108847 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3O)CC2)ccc1O 10.1039/C1MD00140J
44610361 123470 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 14 5 9 4.9 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc(C(O)(c6ccccc6)c6ccccc6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629357 123470 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 14 5 9 4.9 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc(C(O)(c6ccccc6)c6ccccc6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
10622718 38166 0 None 7 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 434 6 2 3 4.5 O=C(NC1CCN(CC2CCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL146359 38166 0 None 7 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 434 6 2 3 4.5 O=C(NC1CCN(CC2CCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
44364174 121471 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 400 7 3 4 3.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@H](O)C2)CC1 10.1021/jm0003135
CHEMBL359220 121471 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 400 7 3 4 3.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@H](O)C2)CC1 10.1021/jm0003135
44593619 186877 0 None -2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493980 186877 0 None -2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
16124708 136812 0 None 28 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 0 2 5.0 CN1C(=O)N(C2CCN(Cc3ccccc3)CC2)CC1(c1ccccc1)c1ccccc1 10.1021/jm061159a
CHEMBL375277 136812 0 None 28 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 0 2 5.0 CN1C(=O)N(C2CCN(Cc3ccccc3)CC2)CC1(c1ccccc1)c1ccccc1 10.1021/jm061159a
44304818 201615 0 None -67 7 Rat 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64788 201615 0 None -67 7 Rat 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
44304818 201615 0 None -67 7 Human 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64788 201615 0 None -67 7 Human 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
11012653 120307 0 None -12 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 6 0 2 4.9 CC(C1=C(CCN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL355769 120307 0 None -12 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 6 0 2 4.9 CC(C1=C(CCN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
4715419 188155 30 None -4 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc(C2CCCN2)o1 10.1021/jm800145d
CHEMBL505086 188155 30 None -4 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc(C2CCCN2)o1 10.1021/jm800145d
134272502 175734 0 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4514058 175734 0 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4595246 175734 0 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
72064 77994 9 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 318 8 0 4 3.1 CCN(CC)CCOC(=O)C(c1ccccc1)N1CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL2110892 77994 9 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 318 8 0 4 3.1 CCN(CC)CCOC(=O)C(c1ccccc1)N1CCCCC1 10.1016/j.bmc.2013.01.072
156017826 177284 0 None -8 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4644285 177284 0 None -8 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
71461680 79125 0 None -2 2 Rat 4.7 pKi = 4.7 Binding
Inhibition of [3H]QNB binding to m3 receptor transfected with CHO cellInhibition of [3H]QNB binding to m3 receptor transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)O[C@H]1CC2CC1N(Cc1ccccc1)C2 10.1021/jm00090a006
CHEMBL2114059 79125 0 None -2 2 Rat 4.7 pKi = 4.7 Binding
Inhibition of [3H]QNB binding to m3 receptor transfected with CHO cellInhibition of [3H]QNB binding to m3 receptor transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)O[C@H]1CC2CC1N(Cc1ccccc1)C2 10.1021/jm00090a006
100 3745 52 None -8 55 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3745 52 None -8 55 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3745 52 None -8 55 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3745 52 None -8 55 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3745 52 None -8 55 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
44431376 86889 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 344 6 1 4 2.7 CN(C)C1(CNCCc2ccccc2F)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL233200 86889 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 344 6 1 4 2.7 CN(C)C1(CNCCc2ccccc2F)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
53325550 58220 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 395 9 2 4 4.9 NCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683924 58220 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 395 9 2 4 4.9 NCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
138680294 177756 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 354 3 2 1 3.9 C[N+]12CCC(CC1)[C@@H](NC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4637749 177756 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 354 3 2 1 3.9 C[N+]12CCC(CC1)[C@@H](NC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4651167 177756 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 354 3 2 1 3.9 C[N+]12CCC(CC1)[C@@H](NC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
155554149 174874 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 4 0 5 3.7 O=C(OCc1ccc2c(c1)OCO2)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4576768 174874 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 4 0 5 3.7 O=C(OCc1ccc2c(c1)OCO2)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
140844412 175854 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3cccc(C(F)(F)F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4441041 175854 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3cccc(C(F)(F)F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596190 175854 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3cccc(C(F)(F)F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
10597259 118752 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 402 7 2 3 3.9 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@H](F)C2)CC1 10.1021/jm0003135
CHEMBL343644 118752 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 402 7 2 3 3.9 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@H](F)C2)CC1 10.1021/jm0003135
145960466 160976 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4128341 160976 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
10572658 121466 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2ccncc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL359197 121466 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2ccncc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
21855 83830 35 None -14 6 Human 6.7 pKi = 6.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1016/s0960-894x(01)00186-x
CHEMBL22108 83830 35 None -14 6 Human 6.7 pKi = 6.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1016/s0960-894x(01)00186-x
578009 119503 1 None - 1 Rat 5.7 pKi = 5.7 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 393 10 1 4 3.4 CN(CC#CCN1CCCC1)C(=O)CCCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
CHEMBL1202052 119503 1 None - 1 Rat 5.7 pKi = 5.7 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 393 10 1 4 3.4 CN(CC#CCN1CCCC1)C(=O)CCCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
CHEMBL350134 119503 1 None - 1 Rat 5.7 pKi = 5.7 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 393 10 1 4 3.4 CN(CC#CCN1CCCC1)C(=O)CCCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
11099206 120274 0 None -4 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 318 5 0 2 4.7 CC(C1=C(CCN2CCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL355455 120274 0 None -4 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 318 5 0 2 4.7 CC(C1=C(CCN2CCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
118719926 115280 0 None -436 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 115280 0 None -436 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
44593618 186876 0 None -4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493979 186876 0 None -4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44299616 194035 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL55698 194035 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
10474335 193025 16 None -676 10 Human 4.7 pKi = 4.7 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
CHEMBL53325 193025 16 None -676 10 Human 4.7 pKi = 4.7 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
611101 202181 2 None -1 4 Rat 5.7 pKi = 5.7 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 380 4 2 6 0.9 NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL68771 202181 2 None -1 4 Rat 5.7 pKi = 5.7 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 380 4 2 6 0.9 NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
44337748 9305 0 None 1 2 Rat 4.7 pKi = 4.7 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL111529 9305 0 None 1 2 Rat 4.7 pKi = 4.7 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
168277127 189993 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 516 9 2 6 4.9 COc1cc(C(=O)O)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
CHEMBL5180420 189993 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 516 9 2 6 4.9 COc1cc(C(=O)O)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
118719928 115282 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354075 115282 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
44593620 187353 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496915 187353 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
137628879 160425 0 None -66 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 950 16 3 9 8.1 CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1 10.1021/acs.jmedchem.6b01892
CHEMBL4068393 160425 0 None -66 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 950 16 3 9 8.1 CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1 10.1021/acs.jmedchem.6b01892
CHEMBL4079233 160425 0 None -66 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 950 16 3 9 8.1 CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1 10.1021/acs.jmedchem.6b01892
CHEMBL4115977 160425 0 None -66 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 950 16 3 9 8.1 CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1 10.1021/acs.jmedchem.6b01892
16094793 82909 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
CHEMBL219118 82909 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
16094810 137360 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1 10.1021/jm0606995
CHEMBL376295 137360 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1 10.1021/jm0606995
250 3334 5 None -56234 13 Human 5.7 pKi = 5.7 Binding
Compound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assayCompound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
5311416 3334 5 None -56234 13 Human 5.7 pKi = 5.7 Binding
Compound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assayCompound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
CHEMBL69733 3334 5 None -56234 13 Human 5.7 pKi = 5.7 Binding
Compound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assayCompound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
156011518 177763 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4637731 177763 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651208 177763 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
10398077 9240 0 None - 1 Rat 4.7 pKi = 4.7 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heartThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heart
ChEMBL 206 2 0 3 1.6 CC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
CHEMBL111123 9240 0 None - 1 Rat 4.7 pKi = 4.7 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heartThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heart
ChEMBL 206 2 0 3 1.6 CC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
10398077 9240 0 None - 1 Rat 4.7 pKi = 4.7 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary glandThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary gland
ChEMBL 206 2 0 3 1.6 CC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
CHEMBL111123 9240 0 None - 1 Rat 4.7 pKi = 4.7 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary glandThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary gland
ChEMBL 206 2 0 3 1.6 CC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
10503358 38450 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3
ChEMBL 442 6 2 3 4.4 Cc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
CHEMBL146567 38450 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3
ChEMBL 442 6 2 3 4.4 Cc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
10497101 70125 0 None -1 3 Rat 8.7 pKi = 8.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 336 4 1 3 3.6 O=C(NC(c1ccccc1)c1ccccc1)OC1CN2CCC1CC2 10.1021/jm050099q
CHEMBL194628 70125 0 None -1 3 Rat 8.7 pKi = 8.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 336 4 1 3 3.6 O=C(NC(c1ccccc1)c1ccccc1)OC1CN2CCC1CC2 10.1021/jm050099q
90666112 108856 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 18 6 9 7.2 Cc1ccc(-c2ccc(O)c(Cl)c2)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c1 10.1039/C1MD00140J
CHEMBL3219044 108856 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 18 6 9 7.2 Cc1ccc(-c2ccc(O)c(Cl)c2)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c1 10.1039/C1MD00140J
90666116 108861 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 19 6 9 7.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219049 108861 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 19 6 9 7.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
44386115 130916 0 None 8 5 Human 8.7 pKi = 8.7 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 650 16 3 4 6.2 O=C(CCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL369062 130916 0 None 8 5 Human 8.7 pKi = 8.7 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 650 16 3 4 6.2 O=C(CCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
16721019 87558 0 None -1 3 Human 8.7 pKi = 8.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 362 7 2 5 2.5 CN(C)C1(CNCCC2CCC(CO)CC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234258 87558 0 None -1 3 Human 8.7 pKi = 8.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 362 7 2 5 2.5 CN(C)C1(CNCCC2CCC(CO)CC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
53372938 128780 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 128780 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
688520 35187 3 None -4 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
CHEMBL1437876 35187 3 None -4 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
CHEMBL3289390 35187 3 None -4 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
174174 519 46 None -2 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
260 519 46 None -2 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
320 519 46 None -2 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
CHEMBL517712 519 46 None -2 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
DB00572 519 46 None -2 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
16115797 137627 0 None -6 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL376870 137627 0 None -6 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
56965018 76828 0 None 2 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042552 76828 0 None 2 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078967 76828 0 None 2 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
11006792 78512 0 None 5 5 Human 8.7 pKi = 8.7 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 648 12 2 4 5.9 O=C(CNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112961 78512 0 None 5 5 Human 8.7 pKi = 8.7 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 648 12 2 4 5.9 O=C(CNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
90666102 108845 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)cc3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219032 108845 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)cc3)CC2)ccc1O 10.1039/C1MD00140J
54757772 65659 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 675 16 5 9 6.0 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Oc4nn(-c5c(O)cccc5F)c5c4CCCC5)CC3)ccc(O)c2[nH]1 10.1021/jm2007535
CHEMBL1836647 65659 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 675 16 5 9 6.0 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Oc4nn(-c5c(O)cccc5F)c5c4CCCC5)CC3)ccc(O)c2[nH]1 10.1021/jm2007535
138680039 176477 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 339 3 2 2 3.7 O=C(Nc1ccc(F)cc1-c1ccccc1)N[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4632615 176477 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 339 3 2 2 3.7 O=C(Nc1ccc(F)cc1-c1ccccc1)N[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
140844416 176032 0 None -12 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3ccc(C(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4516342 176032 0 None -12 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3ccc(C(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597717 176032 0 None -12 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3ccc(C(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
10621363 121176 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)c1 10.1021/jm0003135
CHEMBL358726 121176 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)c1 10.1021/jm0003135
16125620 84224 0 None 93 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 2 4.9 Cc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL222388 84224 0 None 93 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 2 4.9 Cc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
44415886 79425 0 None 74 4 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 607 8 2 4 4.3 CC(C)NC(=O)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL212141 79425 0 None 74 4 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 607 8 2 4 4.3 CC(C)NC(=O)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
16115796 136693 0 None -3 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL375073 136693 0 None -3 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
44406316 72377 0 None 15 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 341 6 1 3 3.6 CCCCCC(O)(C#CC1(OC)CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2005.09.079
CHEMBL199821 72377 0 None 15 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 341 6 1 3 3.6 CCCCCC(O)(C#CC1(OC)CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2005.09.079
44431382 87593 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 332 6 1 4 3.3 CN(C)C1(CNCCC2CCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234438 87593 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 332 6 1 4 3.3 CN(C)C1(CNCCC2CCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
53319787 58225 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 465 14 2 4 6.8 NCCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683929 58225 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 465 14 2 4 6.8 NCCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
54757668 65658 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 331 3 2 5 2.7 Oc1cccc(F)c1-n1nc(OC2CCNCC2)c2c1CCCC2 10.1021/jm2007535
CHEMBL1836646 65658 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 331 3 2 5 2.7 Oc1cccc(F)c1-n1nc(OC2CCNCC2)c2c1CCCC2 10.1021/jm2007535
1734 116 8 None 1 12 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
307 116 8 None 1 12 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL168067 116 8 None 1 12 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
319 1297 39 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
321 1297 39 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
444031 1297 39 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
784 1297 39 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
CHEMBL1346 1297 39 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
DB00496 1297 39 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
10500741 38310 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 392 6 2 3 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL146464 38310 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 392 6 2 3 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL5076445 212670 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44233190 102927 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084679 102927 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
44233192 106000 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084643 106000 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3140141 106000 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
10155225 95396 0 None 2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 3 3.6 COC1(C#CC(C#N)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL258959 95396 0 None 2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 3 3.6 COC1(C#CC(C#N)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
44449463 95659 0 None 12 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 381 3 1 3 4.3 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL260228 95659 0 None 12 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 381 3 1 3 4.3 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
44319339 204191 0 None 44 2 Human 8.6 pKi = 8.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 386 5 1 3 4.7 O=C(c1ccccc1)N(c1ccc(O)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL83982 204191 0 None 44 2 Human 8.6 pKi = 8.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 386 5 1 3 4.7 O=C(c1ccccc1)N(c1ccc(O)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
16125373 84366 0 None 28 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 2 5.2 O=C1NC(c2ccccc2)(C2CCCCC2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL223267 84366 0 None 28 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 2 5.2 O=C1NC(c2ccccc2)(C2CCCCC2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
53326340 58226 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 479 15 2 4 7.2 NCCCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683930 58226 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 479 15 2 4 7.2 NCCCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
155541812 172481 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 5 0 3 4.1 O=C(OC1CN2CCC1CC2)N(CCc1ccc(F)cc1)c1ccccc1 10.1016/j.bmcl.2018.12.022
CHEMBL4519301 172481 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 5 0 3 4.1 O=C(OC1CN2CCC1CC2)N(CCc1ccc(F)cc1)c1ccccc1 10.1016/j.bmcl.2018.12.022
140844401 176113 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3ccc(Br)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4539799 176113 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3ccc(Br)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4598363 176113 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3ccc(Br)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
10470 2453 5 None -11 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2014.04.029
1689 2453 5 None -11 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2014.04.029
4057 2453 5 None -11 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2014.04.029
CHEMBL524004 2453 5 None -11 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2014.04.029
DB04843 2453 5 None -11 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2014.04.029
16125698 84133 0 None 102 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 477 6 1 3 3.7 C[N+]1(CC(=O)c2ccccn2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222054 84133 0 None 102 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 477 6 1 3 3.7 C[N+]1(CC(=O)c2ccccn2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
44431383 87594 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 346 6 1 4 3.7 CN(C)C1(CNCCC2CCCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234439 87594 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 346 6 1 4 3.7 CN(C)C1(CNCCC2CCCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
16125374 84308 0 None 36 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 423 5 1 4 4.7 O=C1NC(c2cccs2)(c2cccs2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL222860 84308 0 None 36 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 423 5 1 4 4.7 O=C1NC(c2cccs2)(c2cccs2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
156011670 177742 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 391 4 1 2 5.2 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636887 177742 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 391 4 1 2 5.2 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
CHEMBL4651086 177742 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 391 4 1 2 5.2 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
16124707 137618 0 None 67 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 5 1 4 4.9 O=C1NC(c2cccs2)(c2cccs2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
CHEMBL376781 137618 0 None 67 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 5 1 4 4.9 O=C1NC(c2cccs2)(c2cccs2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
9846311 202313 8 None -1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 444 6 3 5 3.1 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1016/s0960-894x(03)00350-0
CHEMBL69678 202313 8 None -1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 444 6 3 5 3.1 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1016/s0960-894x(03)00350-0
16125372 84231 0 None 74 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 447 5 1 2 4.9 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL222424 84231 0 None 74 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 447 5 1 2 4.9 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
134272441 175752 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 458 8 1 4 4.2 O=C(OC1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4442329 175752 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 458 8 1 4 4.2 O=C(OC1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4595412 175752 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 458 8 1 4 4.2 O=C(OC1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
16086065 79387 0 None 53 4 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 622 10 3 5 3.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL211976 79387 0 None 53 4 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 622 10 3 5 3.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
9846311 202313 8 None -1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 5 3.1 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1021/jm0003135
CHEMBL69678 202313 8 None -1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 5 3.1 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1021/jm0003135
9936450 34929 0 None -3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm501173q
CHEMBL143469 34929 0 None -3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm501173q
44308912 102360 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 4 2 3 2.1 NCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)C1 10.1016/s0960-894x(03)00350-0
CHEMBL305531 102360 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 4 2 3 2.1 NCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)C1 10.1016/s0960-894x(03)00350-0
44431389 145618 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 348 6 2 5 2.3 CN(C)C1(CNCCC2CCC(O)CC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL391977 145618 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 348 6 2 5 2.3 CN(C)C1(CNCCC2CCC(O)CC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
12872437 11953 0 None -2 5 Rat 8.5 pKi = 8.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 338 2 0 3 3.1 C[N+]1(C)CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00403-G
CHEMBL1183585 11953 0 None -2 5 Rat 8.5 pKi = 8.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 338 2 0 3 3.1 C[N+]1(C)CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00403-G
CHEMBL306182 11953 0 None -2 5 Rat 8.5 pKi = 8.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 338 2 0 3 3.1 C[N+]1(C)CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00403-G
44406476 139994 0 None 15 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 326 3 1 4 2.2 COC1(C#CC(O)(c2ccccn2)C2CCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL381020 139994 0 None 15 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 326 3 1 4 2.2 COC1(C#CC(O)(c2ccccn2)C2CCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44431367 87554 0 None 4 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 326 6 1 4 2.6 CN(C)C1(CNCCc2ccccc2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234252 87554 0 None 4 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 326 6 1 4 2.6 CN(C)C1(CNCCc2ccccc2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
44431370 87556 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 360 6 1 4 3.2 CN(C)C1(CNCCc2ccc(Cl)cc2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234254 87556 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 360 6 1 4 3.2 CN(C)C1(CNCCc2ccc(Cl)cc2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
10214932 86799 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 4 3.5 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C)C1 10.1016/j.bmcl.2007.03.047
CHEMBL232860 86799 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 4 3.5 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C)C1 10.1016/j.bmcl.2007.03.047
9868297 93680 0 None 13 2 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 448 7 2 5 3.1 O=C(N[C@H]1[C@@H]2CN(CCc3ccc4c(c3)OCO4)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL249205 93680 0 None 13 2 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 448 7 2 5 3.1 O=C(N[C@H]1[C@@H]2CN(CCc3ccc4c(c3)OCO4)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
155529196 170844 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 4 0 3 4.4 Cc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
CHEMBL4462631 170844 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 4 0 3 4.4 Cc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
140844398 175787 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3cccc(Br)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4470924 175787 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3cccc(Br)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4595692 175787 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3cccc(Br)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
71452793 79245 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 4 5.1 COc1ccc([S@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2115127 79245 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 4 5.1 COc1ccc([S@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
44430464 91875 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 364 3 0 4 3.6 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(Br)C1 10.1016/j.bmcl.2007.03.047
CHEMBL242823 91875 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 364 3 0 4 3.6 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(Br)C1 10.1016/j.bmcl.2007.03.047
44430467 151557 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 304 3 0 4 3.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(F)C1 10.1016/j.bmcl.2007.03.047
CHEMBL396761 151557 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 304 3 0 4 3.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(F)C1 10.1016/j.bmcl.2007.03.047
44409797 140044 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 294 6 2 4 3.8 Cc1c(NCc2ccccc2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL381259 140044 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 294 6 2 4 3.8 Cc1c(NCc2ccccc2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
137628788 160445 0 None -2 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CC([N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4085150 160445 0 None -2 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CC([N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116149 160445 0 None -2 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CC([N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
138710938 176679 0 None 7 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 353 4 2 4 3.9 N#Cc1ccc(-c2cc(F)ccc2NC(=O)OCC2CCNCC2)cc1 10.1021/acs.jmedchem.0c00297
CHEMBL4636009 176679 0 None 7 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 353 4 2 4 3.9 N#Cc1ccc(-c2cc(F)ccc2NC(=O)OCC2CCNCC2)cc1 10.1021/acs.jmedchem.0c00297
44328561 205635 0 None -4 3 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 243 3 0 3 2.5 COc1ccccc1C(=O)C1=CN2CCC1CC2 10.1016/S0960-894X(01)80824-6
CHEMBL93709 205635 0 None -4 3 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 243 3 0 3 2.5 COc1ccccc1C(=O)C1=CN2CCC1CC2 10.1016/S0960-894X(01)80824-6
2551 782 23 None -346 11 Human 4.7 pKi = 4.7 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
298 782 23 None -346 11 Human 4.7 pKi = 4.7 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
488 782 23 None -346 11 Human 4.7 pKi = 4.7 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
CHEMBL965 782 23 None -346 11 Human 4.7 pKi = 4.7 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
DB00411 782 23 None -346 11 Human 4.7 pKi = 4.7 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
137629259 160457 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 2 0 1 1.8 COc1cccc(C#CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4092769 160457 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 2 0 1 1.8 COc1cccc(C#CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116203 160457 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 2 0 1 1.8 COc1cccc(C#CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
9906447 193904 1 None -281 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant M3 receptorBinding affinity to human recombinant M3 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031738 193904 1 None -281 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant M3 receptorBinding affinity to human recombinant M3 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL555146 193904 1 None -281 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant M3 receptorBinding affinity to human recombinant M3 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
11112362 4890 0 None -1 5 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 410 3 1 3 5.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(Cc5ccccc5)c34)OC21 10.1021/jm011116o
CHEMBL104804 4890 0 None -1 5 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 410 3 1 3 5.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(Cc5ccccc5)c34)OC21 10.1021/jm011116o
16125622 84341 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 495 6 1 3 5.5 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 10.1021/jm061159a
CHEMBL223030 84341 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 495 6 1 3 5.5 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 10.1021/jm061159a
16125329 84511 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 338 6 1 1 3.1 C[N+](C)(C)CCCN1CC(c2ccccc2)(c2ccccc2)NC1=O 10.1021/jm061160+
CHEMBL223724 84511 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 338 6 1 1 3.1 C[N+](C)(C)CCCN1CC(c2ccccc2)(c2ccccc2)NC1=O 10.1021/jm061160+
44593623 187297 0 None -4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496503 187297 0 None -4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539373 187297 0 None -4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
107867 2927 48 None -16 10 Human 5.7 pKi = 5.7 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
309 2927 48 None -16 10 Human 5.7 pKi = 5.7 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
CHEMBL17045 2927 48 None -16 10 Human 5.7 pKi = 5.7 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
10066972 98299 0 None -6 5 Human 5.7 pKi = 5.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL278074 98299 0 None -6 5 Human 5.7 pKi = 5.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
9968046 196486 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL57485 196486 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
10066369 119752 0 None -67 6 Human 4.7 pKi = 4.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 119752 0 None -67 6 Human 4.7 pKi = 4.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
71452384 83383 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
CHEMBL2205816 83383 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
71452384 83383 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
CHEMBL2205816 83383 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
11610557 71687 0 None -8 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1CC(O)c2ccccc2C1c1ccccc1 10.1021/jm050099q
CHEMBL197588 71687 0 None -8 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1CC(O)c2ccccc2C1c1ccccc1 10.1021/jm050099q
11526446 200119 0 None -2 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccsc1 10.1021/jm050099q
CHEMBL606904 200119 0 None -2 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccsc1 10.1021/jm050099q
10623721 38116 0 None 16 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 457 7 3 4 3.5 NCc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
CHEMBL146307 38116 0 None 16 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 457 7 3 4 3.5 NCc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
156015900 177746 0 None -53 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1687 34 6 18 11.6 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCN4CCC(N5CCC(n6c(=O)[nH]c7ccccc76)CC5)CC4)cc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)c3)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)=[N+](CCCCS(=O)(=O)O)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4643273 177746 0 None -53 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1687 34 6 18 11.6 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCN4CCC(N5CCC(n6c(=O)[nH]c7ccccc76)CC5)CC4)cc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)c3)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)=[N+](CCCCS(=O)(=O)O)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651104 177746 0 None -53 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1687 34 6 18 11.6 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCN4CCC(N5CCC(n6c(=O)[nH]c7ccccc76)CC5)CC4)cc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)c3)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)=[N+](CCCCS(=O)(=O)O)c2ccccc21 10.1021/acs.jmedchem.9b02172
137630995 160594 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 4 0 2 1.6 COc1cccc(C(=O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4102555 160594 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 4 0 2 1.6 COc1cccc(C(=O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4117268 160594 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 4 0 2 1.6 COc1cccc(C(=O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
137630043 160490 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 4 0 1 2.4 COc1cccc(/C=C/C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4099667 160490 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 4 0 1 2.4 COc1cccc(/C=C/C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116455 160490 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 4 0 1 2.4 COc1cccc(/C=C/C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
2812 4711 96 None -22 34 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4711 96 None -22 34 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
15169865 11158 0 None -5 3 Rat 4.7 pKi = 4.7 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL1179079 11158 0 None -5 3 Rat 4.7 pKi = 4.7 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL59085 11158 0 None -5 3 Rat 4.7 pKi = 4.7 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
73347826 92110 0 None -1 7 Human 5.7 pKi = 5.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 266 4 1 2 2.4 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)nc1 10.1016/j.bmc.2013.07.045
CHEMBL2432049 92110 0 None -1 7 Human 5.7 pKi = 5.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 266 4 1 2 2.4 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)nc1 10.1016/j.bmc.2013.07.045
44428745 91745 0 None -35 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 635 23 2 6 7.9 COc1ccccc1CNCCCCCCN1CCC(CCC2CCN(CCCCCCNCc3ccccc3OC)CC2)CC1 10.1016/j.bmc.2007.01.022
CHEMBL242345 91745 0 None -35 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 635 23 2 6 7.9 COc1ccccc1CNCCCCCCN1CCC(CCC2CCN(CCCCCCNCc3ccccc3OC)CC2)CC1 10.1016/j.bmc.2007.01.022
10033774 56252 0 None -53 4 Rat 5.7 pKi = 5.7 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 927 31 0 8 12.0 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
CHEMBL163901 56252 0 None -53 4 Rat 5.7 pKi = 5.7 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 927 31 0 8 12.0 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
44274469 80196 0 None -2 5 Human 4.7 pKi = 4.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21509 80196 0 None -2 5 Human 4.7 pKi = 4.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
57326239 76829 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042551 76829 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078974 76829 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
24894625 9686 0 None -2 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@H]1c1ccco1 10.1021/jm800145d
CHEMBL113580 9686 0 None -2 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@H]1c1ccco1 10.1021/jm800145d
CHEMBL553155 9686 0 None -2 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@H]1c1ccco1 10.1021/jm800145d
46227457 14019 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL1198075 14019 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL594801 14019 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
73346334 92109 0 None -2 7 Human 5.7 pKi = 5.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 265 4 1 1 3.0 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
CHEMBL2432048 92109 0 None -2 7 Human 5.7 pKi = 5.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 265 4 1 1 3.0 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
9308 17572 16 None -234 7 Rat 4.7 pKi = 4.7 Binding
Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm00088a029
CHEMBL1255785 17572 16 None -234 7 Rat 4.7 pKi = 4.7 Binding
Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm00088a029
CHEMBL12587 17572 16 None -234 7 Rat 4.7 pKi = 4.7 Binding
Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm00088a029
CHEMBL292911 17572 16 None -234 7 Rat 4.7 pKi = 4.7 Binding
Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm00088a029
10949838 5150 0 None -72 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 4 0 6 4.4 CCOC(=O)c1c(CC)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106218 5150 0 None -72 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 4 0 6 4.4 CCOC(=O)c1c(CC)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
16125158 84340 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 3 4.1 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL223029 84340 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 3 4.1 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
162658112 180489 0 None -1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 393 2 0 5 4.0 CC(C)(C)OC(=O)N1CCN(CC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.bmcl.2020.127632
CHEMBL4759774 180489 0 None -1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 393 2 0 5 4.0 CC(C)(C)OC(=O)N1CCN(CC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.bmcl.2020.127632
90666108 108850 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)cc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219038 108850 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)cc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
53318454 58204 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 310 3 1 3 4.0 CN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683909 58204 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 310 3 1 3 4.0 CN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16125648 84311 0 None 44 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 477 6 1 3 3.7 C[N+]1(CC(=O)c2cccnc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222874 84311 0 None 44 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 477 6 1 3 3.7 C[N+]1(CC(=O)c2cccnc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
155565074 174912 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 400 6 0 3 4.6 O=C(OCCCc1ccc(F)c(F)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4577453 174912 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 400 6 0 3 4.6 O=C(OCCCc1ccc(F)c(F)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
10501523 40280 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1ccccc1CN1CCC(NC(=O)C(O)(c2ccccc2)C2CCCC2)CC1 10.1021/jm0003135
CHEMBL148310 40280 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1ccccc1CN1CCC(NC(=O)C(O)(c2ccccc2)C2CCCC2)CC1 10.1021/jm0003135
10066369 119752 0 None -67 6 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 119752 0 None -67 6 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
156011605 177708 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.4 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Cc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4638067 177708 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.4 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Cc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650888 177708 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.4 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Cc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
71457690 83384 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205817 83384 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
16125507 165626 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 7 1 3 4.5 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCOc2ccccc2)CC1 10.1021/jm061159a
CHEMBL426393 165626 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 7 1 3 4.5 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCOc2ccccc2)CC1 10.1021/jm061159a
11143997 4953 0 None -32 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 408 3 1 5 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL105122 4953 0 None -32 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 408 3 1 5 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
9911615 98574 0 None -114 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 450 5 0 6 5.5 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(SC)cc2CCN1C3 10.1021/jm011116o
CHEMBL280220 98574 0 None -114 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 450 5 0 6 5.5 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(SC)cc2CCN1C3 10.1021/jm011116o
24894632 188830 2 None -1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc(C2CCCN2C)o1 10.1021/jm800145d
CHEMBL513277 188830 2 None -1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc(C2CCCN2C)o1 10.1021/jm800145d
44431375 86888 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 394 6 1 4 3.9 CN(C)C1(CNCCc2c(Cl)cccc2Cl)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL233199 86888 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 394 6 1 4 3.9 CN(C)C1(CNCCc2c(Cl)cccc2Cl)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
16086021 12209 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL1185033 12209 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL385229 12209 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
44627748 13980 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 332 4 0 1 5.4 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL1197705 13980 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 332 4 0 1 5.4 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL583027 13980 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 332 4 0 1 5.4 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
44627854 196032 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL571341 196032 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
44593620 187353 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496915 187353 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
135494454 172186 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 785 25 5 11 6.7 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL450986 172186 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 785 25 5 11 6.7 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
122194378 123492 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 382 7 1 4 3.6 COc1ccc(CCOC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3629537 123492 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 382 7 1 4 3.6 COc1ccc(CCOC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
137661377 158663 0 None -446 8 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4098720 158663 0 None -446 8 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
156010398 177661 0 None -11 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4633895 177661 0 None -11 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650561 177661 0 None -11 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
44422697 11747 0 None -4 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182277 11747 0 None -4 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL227429 11747 0 None -4 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
132060812 161487 0 None -630 10 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4160064 161487 0 None -630 10 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
171578 12198 5 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 281 3 1 2 2.6 C[N+](C)(C)CC#CCOC(=O)Nc1ccc(Cl)cc1 10.1021/jm0510878
CHEMBL1184962 12198 5 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 281 3 1 2 2.6 C[N+](C)(C)CC#CCOC(=O)Nc1ccc(Cl)cc1 10.1021/jm0510878
CHEMBL380759 12198 5 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 281 3 1 2 2.6 C[N+](C)(C)CC#CCOC(=O)Nc1ccc(Cl)cc1 10.1021/jm0510878
290 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
4022 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
5926 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
CHEMBL40554 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
CHEMBL74300 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
290 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
4022 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
5926 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
CHEMBL40554 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
CHEMBL74300 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
290 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
4022 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
5926 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
CHEMBL40554 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
CHEMBL74300 2438 4 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
156013387 177686 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4638935 177686 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650725 177686 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
9817231 157691 17 None -2 7 Human 4.6 pKi = 4.6 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 282 4 0 3 4.1 CCCN1CCC=C(c2cc(-c3ccc(C)cc3)no2)C1 10.1038/s41586-020-2286-9
CHEMBL4088272 157691 17 None -2 7 Human 4.6 pKi = 4.6 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 282 4 0 3 4.1 CCCN1CCC=C(c2cc(-c3ccc(C)cc3)no2)C1 10.1038/s41586-020-2286-9
10870954 119804 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL352779 119804 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
2733638 11809 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
6508731 11809 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
8030329 11809 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
CHEMBL1182640 11809 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
CHEMBL257643 11809 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
2200 3082 38 None -22 13 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
328 3082 38 None -22 13 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
4848 3082 38 None -22 13 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
CHEMBL9967 3082 38 None -22 13 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
DB00670 3082 38 None -22 13 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
15050941 201972 0 None -1 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 427 4 1 5 3.1 O=C1Nc2cccnc2N(C(=O)CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL67381 201972 0 None -1 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 427 4 1 5 3.1 O=C1Nc2cccnc2N(C(=O)CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm00111a032
44308798 202349 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 434 6 1 3 4.4 O=C(N1CCC(CCN2CCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL69904 202349 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 434 6 1 3 4.4 O=C(N1CCC(CCN2CCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
137628850 160422 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1CC[N+](C)(C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4097248 160422 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1CC[N+](C)(C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4115965 160422 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1CC[N+](C)(C)C2 10.1021/acs.jmedchem.7b01113
44326538 13155 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 339 9 0 3 4.3 CCN(CC)CCOC(=O)C(CC)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL1191560 13155 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 339 9 0 3 4.3 CCN(CC)CCOC(=O)C(CC)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
16125369 165707 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 411 5 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCCN(Cc2ccccc2)C1 10.1021/jm061159a
CHEMBL426890 165707 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 411 5 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCCN(Cc2ccccc2)C1 10.1021/jm061159a
16125257 144143 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 350 3 1 1 3.2 C[N+]1(C)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061160+
CHEMBL390839 144143 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 350 3 1 1 3.2 C[N+]1(C)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061160+
10381417 68326 0 None -1 2 Rat 7.6 pKi = 7.6 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2C)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
CHEMBL192061 68326 0 None -1 2 Rat 7.6 pKi = 7.6 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2C)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
11718570 71858 0 None -8 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 376 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1Cc1ccccc1 10.1021/jm050099q
CHEMBL198065 71858 0 None -8 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 376 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1Cc1ccccc1 10.1021/jm050099q
53326339 58213 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 436 12 1 3 7.5 CCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683918 58213 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 436 12 1 3 7.5 CCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
44409956 76393 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 288 4 1 4 3.9 Cc1c(NC2CC2)nc(C(C)C)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL206714 76393 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 288 4 1 4 3.9 Cc1c(NC2CC2)nc(C(C)C)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
10236511 140052 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C)(C)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL381333 140052 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C)(C)CC1 10.1016/j.bmcl.2006.01.006
44443728 93598 0 None 25 2 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 6 2 3 3.9 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL248809 93598 0 None 25 2 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 6 2 3 3.9 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
9913341 81746 3 None -25 5 Human 7.6 pKi = 7.6 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL216927 81746 3 None -25 5 Human 7.6 pKi = 7.6 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL553058 81746 3 None -25 5 Human 7.6 pKi = 7.6 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
86720832 189374 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 476 8 2 6 4.5 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5170720 189374 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 476 8 2 6 4.5 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
168287048 190911 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc([C@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
CHEMBL5193865 190911 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc([C@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
44319016 204417 0 None 25 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 404 5 0 2 5.7 O=C(c1ccc(Cl)cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL86012 204417 0 None 25 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 404 5 0 2 5.7 O=C(c1ccc(Cl)cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
44319006 204452 0 None 12 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 384 6 0 2 4.9 O=C(Cc1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL86309 204452 0 None 12 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 384 6 0 2 4.9 O=C(Cc1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
10044685 204610 5 None 12 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 370 5 0 2 5.0 O=C(c1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL87302 204610 5 None 12 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 370 5 0 2 5.0 O=C(c1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
42853214 204728 0 None 7 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 376 5 0 3 5.1 O=C(c1cccs1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL88078 204728 0 None 7 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 376 5 0 3 5.1 O=C(c1cccs1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
9913341 81746 3 None -25 5 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 81746 3 None -25 5 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL553058 81746 3 None -25 5 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
11748799 164859 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.3 CN(C)CCC1=C(C(C)(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL423831 164859 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.3 CN(C)CCC1=C(C(C)(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
16125618 168112 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1ccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)cc1 10.1021/jm061159a
CHEMBL436492 168112 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1ccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)cc1 10.1021/jm061159a
155524478 170378 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 412 7 0 4 4.5 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
CHEMBL4455481 170378 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 412 7 0 4 4.5 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
155515982 169443 0 None -100000 17 Human 4.6 pKi = 4.6 Binding
Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 169443 0 None -100000 17 Human 4.6 pKi = 4.6 Binding
Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
137629919 160462 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CCC(C[N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4095626 160462 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CCC(C[N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4116258 160462 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CCC(C[N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
44409744 75198 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 308 6 1 4 3.9 Cc1c(NC2CC2)nc(C2CC2)nc1N(C)Cc1ccccc1 10.1016/j.bmcl.2006.01.006
CHEMBL204471 75198 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 308 6 1 4 3.9 Cc1c(NC2CC2)nc(C2CC2)nc1N(C)Cc1ccccc1 10.1016/j.bmcl.2006.01.006
44409746 76400 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 290 4 1 4 3.4 Fc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL206753 76400 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 290 4 1 4 3.4 Fc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
164616706 187930 0 None -426 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 660 14 6 8 1.7 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4850130 187930 0 None -426 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 660 14 6 8 1.7 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028391 187930 0 None -426 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 660 14 6 8 1.7 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
16094791 82844 0 None -6 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL218755 82844 0 None -6 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
129989 447 41 None -48 9 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00046a021
8584 447 41 None -48 9 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00046a021
CHEMBL43383 447 41 None -48 9 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00046a021
14939897 96101 0 None -199 4 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1113 33 2 12 12.0 COc1ccccc1CN(CCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)Cc1ccccc1OC)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL1201994 96101 0 None -199 4 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1113 33 2 12 12.0 COc1ccccc1CN(CCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)Cc1ccccc1OC)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL262913 96101 0 None -199 4 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1113 33 2 12 12.0 COc1ccccc1CN(CCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)Cc1ccccc1OC)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
11833737 119833 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
CHEMBL352966 119833 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
101720828 96673 0 None -269 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
16147087 96673 0 None -269 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL1202002 96673 0 None -269 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL267643 96673 0 None -269 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
14939895 81707 0 None -549 4 Rat 5.6 pKi = 5.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 993 30 3 11 10.1 COc1ccccc1CNCCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL1201997 81707 0 None -549 4 Rat 5.6 pKi = 5.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 993 30 3 11 10.1 COc1ccccc1CNCCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL216629 81707 0 None -549 4 Rat 5.6 pKi = 5.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 993 30 3 11 10.1 COc1ccccc1CNCCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
7047822 176262 12 None 1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@H]2CCCN2)c1 10.1021/jm800145d
CHEMBL461088 176262 12 None 1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@H]2CCCN2)c1 10.1021/jm800145d
44409787 75347 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 317 5 1 6 3.2 O=[N+]([O-])c1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL204777 75347 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 317 5 1 6 3.2 O=[N+]([O-])c1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44420788 84718 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 452 5 1 1 5.3 C[N+]1(Cc2ccccc2)C2CCC1CC(N1CC(c3ccccc3)(c3ccccc3)NC1=O)C2 10.1021/jm061160+
CHEMBL224965 84718 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 452 5 1 1 5.3 C[N+]1(Cc2ccccc2)C2CCC1CC(N1CC(c3ccccc3)(c3ccccc3)NC1=O)C2 10.1021/jm061160+
275176 89383 1 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 355 8 1 4 3.4 CCN(CC)CCOC(=O)C(O)(c1ccccc1)c1c(C)cccc1C 10.1016/j.bmc.2013.01.072
CHEMBL2377388 89383 1 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 355 8 1 4 3.4 CCN(CC)CCOC(=O)C(O)(c1ccccc1)c1c(C)cccc1C 10.1016/j.bmc.2013.01.072
11498 2970 33 None -38 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1021/jm011116o
4995951 2970 33 None -38 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1021/jm011116o
CHEMBL59898 2970 33 None -38 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1021/jm011116o
47358375 180180 1 None -26 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 4 1 2 2.9 O=C(CCN1CCCc2ccccc21)NC1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4756164 180180 1 None -26 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 4 1 2 2.9 O=C(CCN1CCCc2ccccc21)NC1CCCC1 10.1016/j.bmcl.2020.127632
123603 870 25 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
2684 870 25 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
584 870 25 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
9658 870 25 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
CHEMBL168815 870 25 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
10557581 21574 0 None -489 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL1202001 21574 0 None -489 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL131913 21574 0 None -489 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
162353383 181995 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 4 1 4 2.2 Cn1ccc(NC(=O)CCN2CCCc3ccccc32)n1 10.1016/j.bmcl.2020.127632
CHEMBL4787944 181995 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 4 1 4 2.2 Cn1ccc(NC(=O)CCN2CCCc3ccccc32)n1 10.1016/j.bmcl.2020.127632
11057942 5505 0 None - 1 Human 4.6 pKi = 4.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 378 2 2 5 3.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(O)ccc2C1O3 10.1021/jm011116o
CHEMBL107680 5505 0 None - 1 Human 4.6 pKi = 4.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 378 2 2 5 3.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(O)ccc2C1O3 10.1021/jm011116o
44309209 202620 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 5 2 3 3.7 CC(C)(N)CC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL71483 202620 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 5 2 3 3.7 CC(C)(N)CC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
11552283 71346 0 None -2 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 3 0 4 3.8 O=C(O[C@H]1CN2CCC1CC2)C1CCc2ccccc2N1c1ccccc1 10.1021/jm050099q
CHEMBL196481 71346 0 None -2 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 3 0 4 3.8 O=C(O[C@H]1CN2CCC1CC2)C1CCc2ccccc2N1c1ccccc1 10.1021/jm050099q
90666105 108848 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(F)cc3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219035 108848 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(F)cc3O)CC2)ccc1O 10.1039/C1MD00140J
53372936 128779 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670827 128779 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
16124769 84356 0 None 23 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 6 0 2 5.3 O=C1N(C2CCN(Cc3ccccc3)CC2)CC(c2ccccc2)N1Cc1ccccc1 10.1021/jm061159a
CHEMBL223188 84356 0 None 23 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 6 0 2 5.3 O=C1N(C2CCN(Cc3ccccc3)CC2)CC(c2ccccc2)N1Cc1ccccc1 10.1021/jm061159a
44593625 187547 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498358 187547 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539120 187547 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
155521847 170120 0 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 418 5 0 3 5.3 O=C(OCCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4451770 170120 0 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 418 5 0 3 5.3 O=C(OCCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
23352279 205846 0 None -5 3 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 233 2 0 3 3.0 CC(=O)c1ccc(C2=CN3CCC2CC3)s1 10.1016/S0960-894X(01)80824-6
CHEMBL94921 205846 0 None -5 3 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 233 2 0 3 3.0 CC(=O)c1ccc(C2=CN3CCC2CC3)s1 10.1016/S0960-894X(01)80824-6
44400800 165257 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 366 5 2 3 2.5 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL424832 165257 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 366 5 2 3 2.5 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2005.02.036
11034265 119867 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 310 5 0 2 4.3 CC(C1=C(CCN(C)C)Cc2ccc(F)cc21)c1ccccn1 10.1021/jm020895l
CHEMBL353290 119867 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 310 5 0 2 4.3 CC(C1=C(CCN(C)C)Cc2ccc(F)cc21)c1ccccn1 10.1021/jm020895l
44593622 187213 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL495888 187213 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL556390 187213 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
11048067 5504 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 4 0 6 4.6 CCOC(=O)c1c(C)n(CC)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL107679 5504 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 4 0 6 4.6 CCOC(=O)c1c(C)n(CC)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
145961125 160998 0 None -6 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4128667 160998 0 None -6 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
162353382 181152 0 None -28 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 330 4 1 2 4.6 O=C(CCN1CCCc2ccccc21)Nc1cccc2ccccc12 10.1016/j.bmcl.2020.127632
CHEMBL4777127 181152 0 None -28 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 330 4 1 2 4.6 O=C(CCN1CCCc2ccccc21)Nc1cccc2ccccc12 10.1016/j.bmcl.2020.127632
237 203157 43 None 1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 203157 43 None 1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 203157 43 None 1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 203157 43 None 1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
145960592 160814 0 None -6 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4126071 160814 0 None -6 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
44309790 202027 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)OC1CC2CC1CN2Cc1ccccc1 10.1021/jm00090a006
CHEMBL67700 202027 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)OC1CC2CC1CN2Cc1ccccc1 10.1021/jm00090a006
155523889 175950 0 None -346 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 803 21 9 9 1.8 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4454134 175950 0 None -346 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 803 21 9 9 1.8 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597014 175950 0 None -346 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 803 21 9 9 1.8 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
24894109 188441 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL509202 188441 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL551563 188441 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
92218234 120314 1 None -15 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.1 C[N+](C)(C)C[C@@H]1COCCO1 10.1016/j.bmcl.2014.06.020
CHEMBL3309718 120314 1 None -15 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.1 C[N+](C)(C)C[C@@H]1COCCO1 10.1016/j.bmcl.2014.06.020
CHEMBL3558072 120314 1 None -15 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.1 C[N+](C)(C)C[C@@H]1COCCO1 10.1016/j.bmcl.2014.06.020
10851461 58203 35 None 1 4 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptorDisplacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptor
ChEMBL 296 3 2 3 3.7 O=C(Nc1ccccc1-c1ccccc1)OC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL1683908 58203 35 None 1 4 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptorDisplacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptor
ChEMBL 296 3 2 3 3.7 O=C(Nc1ccccc1-c1ccccc1)OC1CCNCC1 10.1021/acs.jmedchem.0c00297
155550436 175927 0 None -346 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4569639 175927 0 None -346 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596780 175927 0 None -346 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
71461681 79130 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 4 5.1 COc1ccc([S@@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2114067 79130 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 4 5.1 COc1ccc([S@@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
197842 102128 3 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 326 8 0 2 3.8 CC[N+](C)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377385 102128 3 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 326 8 0 2 3.8 CC[N+](C)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL3041160 102128 3 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 326 8 0 2 3.8 CC[N+](C)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
155553089 173533 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 6 0 4 4.5 COc1ccc(CCN(C(=O)OC2C[C@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4545030 173533 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 6 0 4 4.5 COc1ccc(CCN(C(=O)OC2C[C@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
10810094 119055 0 None 15 3 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 384 6 2 3 3.8 O=C(NC1CCN(CC2CCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL345985 119055 0 None 15 3 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 384 6 2 3 3.8 O=C(NC1CCN(CC2CCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
146025727 171119 0 None -100 27 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171119 0 None -100 27 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
71718669 86530 0 None -2 3 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 303 3 0 5 2.0 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323446 86530 0 None -2 3 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 303 3 0 5 2.0 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
44448646 11803 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 1 4.3 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCCCC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182612 11803 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 1 4.3 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCCCC1 10.1016/j.bmcl.2008.03.061
CHEMBL254586 11803 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 1 4.3 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCCCC1 10.1016/j.bmcl.2008.03.061
10969696 131583 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 334 5 0 3 3.9 CC(C1=C(CCN2CCOCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL369575 131583 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 334 5 0 3 3.9 CC(C1=C(CCN2CCOCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
24894628 178544 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCCC1c1ccco1 10.1021/jm800145d
CHEMBL471942 178544 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCCC1c1ccco1 10.1021/jm800145d
CHEMBL554532 178544 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCCC1c1ccco1 10.1021/jm800145d
11101362 5056 0 None -7 5 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Cl)ccc2C1O3 10.1021/jm011116o
CHEMBL105674 5056 0 None -7 5 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Cl)ccc2C1O3 10.1021/jm011116o
44274468 80194 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21508 80194 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
155563061 174729 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 410 7 0 5 4.0 COc1ccc(CCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4573269 174729 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 410 7 0 5 4.0 COc1ccc(CCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
154734599 2467 8 None -19 11 Human 6.6 pKi = 6.6 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
327 2467 8 None -19 11 Human 6.6 pKi = 6.6 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
4108 2467 8 None -19 11 Human 6.6 pKi = 6.6 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
CHEMBL27673 2467 8 None -19 11 Human 6.6 pKi = 6.6 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
71454535 79124 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)O[C@@H]1CC2CC1CN2C 10.1021/jm00090a006
CHEMBL2114058 79124 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)O[C@@H]1CC2CC1CN2C 10.1021/jm00090a006
2200 3082 38 None -22 13 Rat 7.6 pKi = 7.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00059a009
328 3082 38 None -22 13 Rat 7.6 pKi = 7.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00059a009
4848 3082 38 None -22 13 Rat 7.6 pKi = 7.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00059a009
CHEMBL9967 3082 38 None -22 13 Rat 7.6 pKi = 7.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00059a009
DB00670 3082 38 None -22 13 Rat 7.6 pKi = 7.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00059a009
10671167 120985 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3
ChEMBL 448 6 2 3 4.9 O=C(NC1CCN(CC2CCCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL358289 120985 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3
ChEMBL 448 6 2 3 4.9 O=C(NC1CCN(CC2CCCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
11695960 72050 0 None -3 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 348 2 0 3 3.8 O=C(O[C@H]1CN2CCC1CC2)N1Cc2ccccc2C1c1ccccc1 10.1021/jm050099q
CHEMBL198669 72050 0 None -3 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 348 2 0 3 3.8 O=C(O[C@H]1CN2CCC1CC2)N1Cc2ccccc2C1c1ccccc1 10.1021/jm050099q
53318455 58227 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 556 10 5 7 4.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683931 58227 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 556 10 5 7 4.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
13981865 112314 2 None -11 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
CHEMBL3289391 112314 2 None -11 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
CHEMBL3306998 112314 2 None -11 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
155535606 171486 0 None -77 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 1077 20 5 12 6.0 CCC(=O)NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.8b01967
CHEMBL4471882 171486 0 None -77 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 1077 20 5 12 6.0 CCC(=O)NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.8b01967
155539713 175786 0 None -245 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4515788 175786 0 None -245 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595691 175786 0 None -245 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
289 240 6 None -257 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 240 6 None -257 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 240 6 None -257 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
155551421 173394 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 424 7 0 5 4.5 COc1ccc(CCN(C(=O)OC2C[C@H]3CC[C@H](C2)N3C)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4541656 173394 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 424 7 0 5 4.5 COc1ccc(CCN(C(=O)OC2C[C@H]3CC[C@H](C2)N3C)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
15629515 38920 3 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 191 1 1 2 1.8 CN(C)C1CCc2cccc(O)c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL146953 38920 3 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 191 1 1 2 1.8 CN(C)C1CCc2cccc(O)c2C1 10.1021/acs.jmedchem.7b01113
44309788 102197 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CC2CC1N(C)C2 10.1021/jm00090a006
CHEMBL304551 102197 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CC2CC1N(C)C2 10.1021/jm00090a006
10871551 120003 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 340 6 0 2 5.2 CCC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
CHEMBL354523 120003 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 340 6 0 2 5.2 CCC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
44593616 192611 0 None -4 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL523518 192611 0 None -4 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
10139614 4962 0 None -19 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 462 8 1 5 5.9 CCCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL105160 4962 0 None -19 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 462 8 1 5 5.9 CCCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
16125531 83938 0 None 3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CC[C@@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL221775 83938 0 None 3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CC[C@@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
71575447 85775 0 None -46 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 363 5 0 4 3.5 CN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
CHEMBL2312361 85775 0 None -46 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 363 5 0 4 3.5 CN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
11011757 58911 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 291 5 0 1 4.8 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccc1 10.1021/jm020895l
CHEMBL170221 58911 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 291 5 0 1 4.8 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccc1 10.1021/jm020895l
44593624 187546 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498357 187546 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL554916 187546 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
109013312 179554 1 None -10 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 3 0 2 2.5 O=C(CCN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4748774 179554 1 None -10 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 3 0 2 2.5 O=C(CCN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
109032820 182293 1 None -7 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCCN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
CHEMBL4791819 182293 1 None -7 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCCN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
24894633 176326 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@H]2CCCN2C)o1 10.1021/jm800145d
CHEMBL461709 176326 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@H]2CCCN2C)o1 10.1021/jm800145d
16086031 11723 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 606 10 2 4 4.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL1182134 11723 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 606 10 2 4 4.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL214270 11723 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 606 10 2 4 4.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
9889312 78021 0 None -4 5 Human 7.5 pKi = 7.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 437 6 0 5 4.4 COc1ccc([S@@+]([O-])c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2111540 78021 0 None -4 5 Human 7.5 pKi = 7.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 437 6 0 5 4.4 COc1ccc([S@@+]([O-])c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
44309108 102620 0 None 2 3 Human 6.5 pKi = 6.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 372 4 3 3 3.6 O=C(Nc1ccc2c(c1)CNC2)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL307554 102620 0 None 2 3 Human 6.5 pKi = 6.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 372 4 3 3 3.6 O=C(Nc1ccc2c(c1)CNC2)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
155524809 170406 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 5 0 5 3.7 O=C(OCCc1ccc2c(c1)OCO2)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4456047 170406 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 5 0 5 3.7 O=C(OCCc1ccc2c(c1)OCO2)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
44400887 70654 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 360 5 2 3 2.0 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.02.036
CHEMBL195169 70654 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 360 5 2 3 2.0 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.02.036
6338102 99999 1 None -20 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL290723 99999 1 None -20 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL59587 99999 1 None -20 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
162353391 180239 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 282 4 1 4 2.3 O=C(CCN1CCCc2ccccc21)Nc1cccnn1 10.1016/j.bmcl.2020.127632
CHEMBL4756873 180239 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 282 4 1 4 2.3 O=C(CCN1CCCc2ccccc21)Nc1cccnn1 10.1016/j.bmcl.2020.127632
135 2496 38 None -22 57 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2496 38 None -22 57 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2496 38 None -22 57 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2496 38 None -22 57 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2496 38 None -22 57 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
71454526 79049 0 None 1 2 Rat 4.5 pKi = 4.5 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@@H]1C[C@@H]2C[C@H](C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL2113669 79049 0 None 1 2 Rat 4.5 pKi = 4.5 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@@H]1C[C@@H]2C[C@H](C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
16125400 84240 0 None 35 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 494 6 1 2 4.5 C[N+]1(CC(=O)c2cccc(F)c2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222449 84240 0 None 35 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 494 6 1 2 4.5 C[N+]1(CC(=O)c2cccc(F)c2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
10628017 21516 0 None -8 5 Rat 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 650 26 3 7 7.0 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL131865 21516 0 None -8 5 Rat 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 650 26 3 7 7.0 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
90666123 108869 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 752 16 6 10 6.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
CHEMBL3219056 108869 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 752 16 6 10 6.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
10551354 39519 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 446 6 2 3 4.2 O=C(NC1CCN(Cc2cccc(F)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL147611 39519 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 446 6 2 3 4.2 O=C(NC1CCN(Cc2cccc(F)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
315401 89382 3 None -2 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 343 8 1 4 3.5 CCN(CC)CCSC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377387 89382 3 None -2 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 343 8 1 4 3.5 CCN(CC)CCSC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
16125567 84334 0 None 104 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
CHEMBL223016 84334 0 None 104 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
2745 3800 39 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572 3800 39 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
66007 3800 39 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
7315 3800 39 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
CHEMBL1490 3800 39 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
DB00376 3800 39 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
10125445 75675 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to muscarinic M3 receptorsBinding affinity to muscarinic M3 receptors
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205654 75675 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to muscarinic M3 receptorsBinding affinity to muscarinic M3 receptors
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL5077250 212717 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3cccc(C(F)F)c3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
168275473 189843 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 490 8 2 7 3.6 Cn1nc(COc2cccc([C@@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1C(=O)O 10.1021/acs.jmedchem.2c00609
CHEMBL5178217 189843 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 490 8 2 7 3.6 Cn1nc(COc2cccc([C@@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1C(=O)O 10.1021/acs.jmedchem.2c00609
168276300 189915 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 487 8 2 6 4.3 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)nc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5179380 189915 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 487 8 2 6 4.3 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)nc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
69058946 105993 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084658 105993 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3140110 105993 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
10125445 75675 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
CHEMBL205654 75675 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
118737354 118555 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 703 12 6 8 5.8 Cc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426701 118555 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 703 12 6 8 5.8 Cc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
2705 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.09.079
360 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.09.079
443879 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.09.079
CHEMBL1382 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.09.079
DB01036 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.09.079
10269504 133850 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL371734 133850 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
10125445 75675 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
CHEMBL205654 75675 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
10125445 75675 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205654 75675 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
9910802 120497 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 434 6 2 4 4.2 O=C(NC1CCN(Cc2ccsc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL356505 120497 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 434 6 2 4 4.2 O=C(NC1CCN(Cc2ccsc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
44385809 61137 0 None 22 5 Human 8.5 pKi = 8.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 636 15 3 4 5.8 O=C(CCCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL177040 61137 0 None 22 5 Human 8.5 pKi = 8.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 636 15 3 4 5.8 O=C(CCCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
44308733 101720 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 5 2 3 3.3 CC1(CCN)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL302809 101720 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 5 2 3 3.3 CC1(CCN)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
44431381 148489 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 318 6 1 4 2.9 CN(C)C1(CNCCC2CCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL394254 148489 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 318 6 1 4 2.9 CN(C)C1(CNCCC2CCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
44311762 162920 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 440 6 1 5 4.0 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCNCC2)CC1 10.1016/s0960-894x(00)00457-1
CHEMBL420008 162920 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 440 6 1 5 4.0 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCNCC2)CC1 10.1016/s0960-894x(00)00457-1
11561621 200118 0 None -3 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccsc1 10.1021/jm050099q
CHEMBL606903 200118 0 None -3 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccsc1 10.1021/jm050099q
11798126 41728 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 458 7 2 4 4.1 COc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
CHEMBL149484 41728 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 458 7 2 4 4.1 COc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
10693031 120474 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 412 6 2 4 4.2 Cc1cc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)cs1 10.1021/jm0003135
CHEMBL356305 120474 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 412 6 2 4 4.2 Cc1cc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)cs1 10.1021/jm0003135
11501540 133080 0 None -3 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1cccs1 10.1021/jm050099q
CHEMBL371293 133080 0 None -3 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1cccs1 10.1021/jm050099q
2705 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
360 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
443879 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
CHEMBL1382 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
DB01036 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
2705 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2010.10.132
360 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2010.10.132
443879 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2010.10.132
CHEMBL1382 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2010.10.132
DB01036 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2010.10.132
2705 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/jm2007535
360 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/jm2007535
443879 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/jm2007535
CHEMBL1382 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/jm2007535
DB01036 3781 59 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/jm2007535
2705 3781 59 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
360 3781 59 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
443879 3781 59 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
CHEMBL1382 3781 59 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
DB01036 3781 59 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
10834711 120896 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 398 6 2 4 3.9 O=C(NC1CCN(Cc2ccsc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL358193 120896 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 398 6 2 4 3.9 O=C(NC1CCN(Cc2ccsc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
42596929 76835 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042404 76835 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079021 76835 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
9827782 103078 0 None -41 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 512 7 0 6 4.9 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(C(=O)OCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
CHEMBL308566 103078 0 None -41 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 512 7 0 6 4.9 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(C(=O)OCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
9799291 159573 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 5 2 3 2.9 NCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL410890 159573 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 5 2 3 2.9 NCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
90666103 108846 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(O)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219033 108846 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(O)c3)CC2)ccc1O 10.1039/C1MD00140J
44554514 123469 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 692 18 5 9 5.9 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)c5ccccc5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629356 123469 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 692 18 5 9 5.9 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)c5ccccc5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
44609903 123472 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc([C@](O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629359 123472 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc([C@](O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
16086004 138707 0 None 77 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL378885 138707 0 None 77 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
155551383 176050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 582 8 1 3 5.3 O=C(OC1C[N+]2(CCCc3cccc(I)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4541647 176050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 582 8 1 3 5.3 O=C(OC1C[N+]2(CCCc3cccc(I)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597851 176050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 582 8 1 3 5.3 O=C(OC1C[N+]2(CCCc3cccc(I)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
10812455 39549 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 428 6 2 3 4.1 O=C(NC1CCN(Cc2ccccc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL147653 39549 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 428 6 2 3 4.1 O=C(NC1CCN(Cc2ccccc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
16065268 67586 0 None 2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 456 9 1 3 5.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2ccccc2)CC1 10.1021/jm200884j
CHEMBL1910849 67586 0 None 2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 456 9 1 3 5.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2ccccc2)CC1 10.1021/jm200884j
164617537 184630 0 None -100 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4857743 184630 0 None -100 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164627100 185977 0 None -25 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 739 13 6 9 5.8 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmcl.2021.127975
CHEMBL4878138 185977 0 None -25 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 739 13 6 9 5.8 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmcl.2021.127975
90209394 190491 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 493 8 2 7 4.3 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)O)cs2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5187593 190491 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 493 8 2 7 4.3 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)O)cs2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
168287089 190955 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 504 8 2 5 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)c(F)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5194569 190955 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 504 8 2 5 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)c(F)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
10269504 133850 0 None 6 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL371734 133850 0 None 6 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
44318928 204049 0 None 28 2 Human 8.4 pKi = 8.4 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 400 6 0 3 5.0 COc1ccc(N(C(=O)c2ccccc2)C2CCN(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00487-0
CHEMBL82859 204049 0 None 28 2 Human 8.4 pKi = 8.4 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 400 6 0 3 5.0 COc1ccc(N(C(=O)c2ccccc2)C2CCN(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00487-0
44319043 204339 0 None 17 2 Human 8.4 pKi = 8.4 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 410 5 0 3 5.7 O=C(c1cccs1)N(c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85391 204339 0 None 17 2 Human 8.4 pKi = 8.4 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 410 5 0 3 5.7 O=C(c1cccs1)N(c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
2774 3807 92 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
5593 3807 92 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
7319 3807 92 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
CHEMBL1200604 3807 92 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB00809 3807 92 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB01199 3807 92 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
2733619 11806 5 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
6508725 11806 5 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
CHEMBL1182634 11806 5 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
CHEMBL257431 11806 5 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
138710717 177448 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1ccccc1Cl)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4646717 177448 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1ccccc1Cl)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
10574041 39583 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 418 6 2 4 3.7 O=C(NC1CCN(Cc2ccoc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL147695 39583 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 418 6 2 4 3.7 O=C(NC1CCN(Cc2ccoc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
156021441 177580 0 None -6 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4648939 177580 0 None -6 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
155562882 174661 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 350 5 0 3 4.0 O=C(OCCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4571841 174661 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 350 5 0 3 4.0 O=C(OCCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
44318930 105691 0 None -6 4 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
CHEMBL313738 105691 0 None -6 4 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
10235 2636 1 None -1230 6 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M3 receptor (unknown origin)Inhibition of muscarinic M3 receptor (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
137553161 2636 1 None -1230 6 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M3 receptor (unknown origin)Inhibition of muscarinic M3 receptor (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
CHEMBL4470080 2636 1 None -1230 6 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M3 receptor (unknown origin)Inhibition of muscarinic M3 receptor (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
137640201 156419 2 None -2398 13 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156419 2 None -2398 13 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
44593617 186848 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493795 186848 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
10373706 57108 0 None -60 4 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 959 31 2 10 10.2 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
CHEMBL165220 57108 0 None -60 4 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 959 31 2 10 10.2 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
441383 20133 54 None -6 17 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 20133 54 None -6 17 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
11808946 120124 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL354678 120124 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
135430667 4889 0 None -50 5 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 402 2 1 6 4.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(-c5nc(C)no5)c34)OC21 10.1021/jm011116o
CHEMBL104803 4889 0 None -50 5 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 402 2 1 6 4.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(-c5nc(C)no5)c34)OC21 10.1021/jm011116o
15157139 99350 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 331 8 0 3 4.4 CN(C)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL285440 99350 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 331 8 0 3 4.4 CN(C)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
10410916 93636 0 None 9 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 438 7 2 3 4.0 O=C(N[C@H]1[C@@H]2CN(CCc3ccc(Cl)cc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL249007 93636 0 None 9 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 438 7 2 3 4.0 O=C(N[C@H]1[C@@H]2CN(CCc3ccc(Cl)cc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
11808040 167831 0 None -2 6 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 4 0 2 3.8 CC(C1=C(CN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL434684 167831 0 None -2 6 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 4 0 2 3.8 CC(C1=C(CN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
25034182 172015 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL448870 172015 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL540359 172015 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
44319017 204586 0 None 19 2 Human 7.5 pKi = 7.5 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 448 5 0 2 5.8 O=C(c1ccc(Br)cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL87132 204586 0 None 19 2 Human 7.5 pKi = 7.5 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 448 5 0 2 5.8 O=C(c1ccc(Br)cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
44443722 154381 0 None 29 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 6 2 3 3.7 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL400953 154381 0 None 29 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 6 2 3 3.7 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.06.081
16125325 84150 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 336 3 1 1 2.8 C[N+]1(C)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222090 84150 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 336 3 1 1 2.8 C[N+]1(C)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
535891 119368 2 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 279 8 1 3 1.5 CN(CC#CCN1CCCC1)C(=O)CCCCCCN 10.1021/jm00164a044
CHEMBL1202131 119368 2 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 279 8 1 3 1.5 CN(CC#CCN1CCCC1)C(=O)CCCCCCN 10.1021/jm00164a044
CHEMBL348946 119368 2 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 279 8 1 3 1.5 CN(CC#CCN1CCCC1)C(=O)CCCCCCN 10.1021/jm00164a044
71575122 85786 0 None -134 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 377 6 0 4 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
CHEMBL2312376 85786 0 None -134 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 377 6 0 4 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
12488 1627 51 None -8 23 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1627 51 None -8 23 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1627 51 None -8 23 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1627 51 None -8 23 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
16125327 84327 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CC[C@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222975 84327 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CC[C@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
44409749 76191 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 350 4 1 4 4.1 Brc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL206127 76191 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 350 4 1 4 4.1 Brc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44409962 76962 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 320 4 1 4 3.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCc2ccccc2C1 10.1016/j.bmcl.2006.01.006
CHEMBL208299 76962 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 320 4 1 4 3.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCc2ccccc2C1 10.1016/j.bmcl.2006.01.006
44409760 138133 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 5 2 4 4.0 Cc1c(NC2CCCCC2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL377728 138133 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 5 2 4 4.0 Cc1c(NC2CCCCC2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
44418764 81747 0 None -8 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 81747 0 None -8 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
10109893 81753 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
CHEMBL216983 81753 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
CHEMBL544840 81753 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
11131099 119755 0 None -3 5 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
CHEMBL352404 119755 0 None -3 5 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
10337773 101114 0 None -79 10 Human 4.5 pKi = 4.5 Binding
Binding affinity against Muscarinic M3 receptorBinding affinity against Muscarinic M3 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
CHEMBL298612 101114 0 None -79 10 Human 4.5 pKi = 4.5 Binding
Binding affinity against Muscarinic M3 receptorBinding affinity against Muscarinic M3 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
162353372 180805 0 None -8 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.2 O=C(CCN1CCCc2ccccc21)N1CCCCC1CO 10.1016/j.bmcl.2020.127632
CHEMBL4763422 180805 0 None -8 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.2 O=C(CCN1CCCc2ccccc21)N1CCCCC1CO 10.1016/j.bmcl.2020.127632
57326146 76834 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042403 76834 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079020 76834 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccccc2)O1 10.1021/jm2013216
2750 202363 69 None -1 12 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 202363 69 None -1 12 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
53319788 58234 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 624 17 5 6 5.4 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)C1 10.1016/j.bmcl.2011.01.043
CHEMBL1683939 58234 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 624 17 5 6 5.4 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)C1 10.1016/j.bmcl.2011.01.043
44430461 167788 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 314 3 0 4 3.9 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C)(C)C1 10.1016/j.bmcl.2007.03.047
CHEMBL434388 167788 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 314 3 0 4 3.9 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C)(C)C1 10.1016/j.bmcl.2007.03.047
44409653 76162 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 270 4 1 4 3.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CC=CCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205992 76162 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 270 4 1 4 3.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CC=CCC1 10.1016/j.bmcl.2006.01.006
44409765 138134 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(NC2CC2)nc([C@@H]2C[C@H]2C)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL377729 138134 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(NC2CC2)nc([C@@H]2C[C@H]2C)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
10830843 202265 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 4 3 3 2.2 O=C(NC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL69383 202265 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 4 3 3 2.2 O=C(NC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
44409557 140476 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 5 2.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(=O)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL382374 140476 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 5 2.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(=O)CC1 10.1016/j.bmcl.2006.01.006
10421982 204322 0 None -5 4 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
CHEMBL85190 204322 0 None -5 4 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
578008 56140 1 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 379 9 1 4 3.0 CN(CC#CCN1CCCC1)C(=O)CCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
CHEMBL1202048 56140 1 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 379 9 1 4 3.0 CN(CC#CCN1CCCC1)C(=O)CCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
CHEMBL163202 56140 1 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 379 9 1 4 3.0 CN(CC#CCN1CCCC1)C(=O)CCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
2274 3124 53 None -21 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3124 53 None -21 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3124 53 None -21 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3124 53 None -21 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3124 53 None -21 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
2551 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44627855 195695 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569212 195695 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
44593624 187546 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498357 187546 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL554916 187546 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44593627 192696 0 None -2 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524071 192696 0 None -2 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL541671 192696 0 None -2 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
162353375 179315 0 None -9 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 4 0 3 1.7 COC1CN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
CHEMBL4745885 179315 0 None -9 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 4 0 3 1.7 COC1CN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
162353384 180508 0 None -6 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC1CO 10.1016/j.bmcl.2020.127632
CHEMBL4760037 180508 0 None -6 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC1CO 10.1016/j.bmcl.2020.127632
46227461 14021 0 None 1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198077 14021 0 None 1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL594803 14021 0 None 1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
122194372 123488 0 None 2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 352 6 1 3 3.0 COc1ccc(CCNC(=O)C2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3629532 123488 0 None 2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 352 6 1 3 3.0 COc1ccc(CCNC(=O)C2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
4841 67089 3 None -3 5 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1889399 67089 3 None -3 5 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1909073 67089 3 None -3 5 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
44443732 93803 0 None 41 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL250030 93803 0 None 41 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
44379508 57856 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 664 9 1 4 6.6 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1)C(=O)c1cccc(I)c1 10.1016/S0960-894X(97)00109-1
CHEMBL168145 57856 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 664 9 1 4 6.6 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1)C(=O)c1cccc(I)c1 10.1016/S0960-894X(97)00109-1
44627742 196700 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 323 4 0 2 5.8 CN1CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL576707 196700 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 323 4 0 2 5.8 CN1CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
9998202 68824 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL192485 68824 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
14939893 9443 0 None -112 5 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL112244 9443 0 None -112 5 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
2719 904 66 None -3 11 Human 5.5 pKi = 5.5 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
5535 904 66 None -3 11 Human 5.5 pKi = 5.5 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
607 904 66 None -3 11 Human 5.5 pKi = 5.5 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
CHEMBL76 904 66 None -3 11 Human 5.5 pKi = 5.5 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
DB00608 904 66 None -3 11 Human 5.5 pKi = 5.5 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
10315426 100579 0 None -10 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL294663 100579 0 None -10 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
162353369 180213 0 None -2 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC(O)CC1 10.1016/j.bmcl.2020.127632
CHEMBL4756442 180213 0 None -2 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC(O)CC1 10.1016/j.bmcl.2020.127632
24894516 172139 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@@H]2CCCN2C)o1 10.1021/jm800145d
CHEMBL450463 172139 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@@H]2CCCN2C)o1 10.1021/jm800145d
16125535 84694 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 324 5 1 1 2.7 C[N+](C)(C)CCN1CC(c2ccccc2)(c2ccccc2)NC1=O 10.1021/jm061160+
CHEMBL224784 84694 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 324 5 1 1 2.7 C[N+](C)(C)CCN1CC(c2ccccc2)(c2ccccc2)NC1=O 10.1021/jm061160+
36381 12833 5 None 1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmcl.2012.08.046
CHEMBL1189234 12833 5 None 1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmcl.2012.08.046
36381 12833 5 None 1 6 Human 6.5 pKi = 6.5 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmc.2013.07.045
CHEMBL1189234 12833 5 None 1 6 Human 6.5 pKi = 6.5 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmc.2013.07.045
118719930 115284 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 470 17 1 3 6.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354077 115284 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 470 17 1 3 6.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCCCO)CC1 10.1021/jm501173q
10225881 107135 0 None -112 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 450 6 1 5 5.9 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL318995 107135 0 None -112 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 450 6 1 5 5.9 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
44337776 110702 0 None -1 2 Rat 5.5 pKi = 5.5 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@H]1CC2CC(C1)N(C(C)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL326453 110702 0 None -1 2 Rat 5.5 pKi = 5.5 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@H]1CC2CC(C1)N(C(C)c1ccccc1)C2 10.1021/jm00115a003
12963076 194950 2 None -8128 6 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL564226 194950 2 None -8128 6 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
24865895 95559 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL259662 95559 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL390842 95559 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
11523051 95842 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 218 1 0 2 0.7 C[C@@H]1O[C@H]([C@@H]2CCC[N+]2(C)C)C[S@@+]1[O-] 10.1021/jm0510878
CHEMBL2093084 95842 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 218 1 0 2 0.7 C[C@@H]1O[C@H]([C@@H]2CCC[N+]2(C)C)C[S@@+]1[O-] 10.1021/jm0510878
CHEMBL261194 95842 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 218 1 0 2 0.7 C[C@@H]1O[C@H]([C@@H]2CCC[N+]2(C)C)C[S@@+]1[O-] 10.1021/jm0510878
44576913 192711 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 336 4 0 2 3.3 C[N+](C)(C)C[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524186 192711 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 336 4 0 2 3.3 C[N+](C)(C)C[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL557808 192711 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 336 4 0 2 3.3 C[N+](C)(C)C[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
2551 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44593621 192694 0 None -2 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524061 192694 0 None -2 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
15050949 202278 0 None -3 3 Rat 5.5 pKi = 5.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 641 10 3 8 4.2 CC(C)(C)OC(=O)NCCCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
CHEMBL69458 202278 0 None -3 3 Rat 5.5 pKi = 5.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 641 10 3 8 4.2 CC(C)(C)OC(=O)NCCCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
44400375 68832 0 None 2 2 Rat 7.5 pKi = 7.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 367 5 1 4 3.0 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL192537 68832 0 None 2 2 Rat 7.5 pKi = 7.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 367 5 1 4 3.0 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2005.02.036
9842753 200127 0 None 1 3 Rat 7.5 pKi = 7.5 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1C[C@@H](O)c2ccccc2[C@@H]1c1ccccc1 10.1021/jm050099q
CHEMBL606963 200127 0 None 1 3 Rat 7.5 pKi = 7.5 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1C[C@@H](O)c2ccccc2[C@@H]1c1ccccc1 10.1021/jm050099q
155567380 175834 0 None -446 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 981 20 7 10 4.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4589047 175834 0 None -446 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 981 20 7 10 4.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596064 175834 0 None -446 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 981 20 7 10 4.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
155520267 169876 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 356 5 0 3 4.1 CN1CCCC(OC(=O)N(CCc2ccc(F)cc2)c2ccccc2)C1 10.1016/j.bmcl.2018.12.022
CHEMBL4448667 169876 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 356 5 0 3 4.1 CN1CCCC(OC(=O)N(CCc2ccc(F)cc2)c2ccccc2)C1 10.1016/j.bmcl.2018.12.022
16125503 84260 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 2 5.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CC2CCCCC2)CC1 10.1021/jm061159a
CHEMBL222527 84260 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 2 5.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CC2CCCCC2)CC1 10.1021/jm061159a
156012936 177721 0 None -5 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4639004 177721 0 None -5 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650969 177721 0 None -5 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
162353386 180398 0 None -3 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 C[C@H]1CCC[C@@H](C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4758635 180398 0 None -3 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 C[C@H]1CCC[C@@H](C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
44422692 11748 0 None -5 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182296 11748 0 None -5 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL228144 11748 0 None -5 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
44446841 12232 0 None -2 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL1185281 12232 0 None -2 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL404557 12232 0 None -2 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
122194380 123493 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 381 7 2 3 3.2 COc1ccc(CCNC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3629539 123493 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 381 7 2 3 3.2 COc1ccc(CCNC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
16125640 84318 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 486 10 1 3 4.3 COCC[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222917 84318 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 486 10 1 3 4.3 COCC[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
2551 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2801 161325 56 None -1 28 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161325 56 None -1 28 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161325 56 None -1 28 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
4543 169982 36 None -3 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169982 36 None -3 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169982 36 None -3 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
90666122 108868 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 738 15 6 10 5.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
CHEMBL3219055 108868 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 738 15 6 10 5.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
44627744 13926 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 348 4 1 2 4.5 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL1197389 13926 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 348 4 1 2 4.5 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL569729 13926 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 348 4 1 2 4.5 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
71457691 83385 0 None -1 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccccc1CN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205823 83385 0 None -1 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccccc1CN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
53414666 158754 7 None -3 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 4 1 3 1.2 c1cncc(COCC2CCNC2)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4099673 158754 7 None -3 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 4 1 3 1.2 c1cncc(COCC2CCNC2)c1 10.1021/acs.jmedchem.7b01113
574782 101681 2 None 1 3 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 397 3 1 6 2.3 CSc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCN(C)CC1 10.1021/jm00111a032
CHEMBL302557 101681 2 None 1 3 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 397 3 1 6 2.3 CSc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCN(C)CC1 10.1021/jm00111a032
44448380 11810 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 436 7 1 1 5.0 C[N+]1(C)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182644 11810 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 436 7 1 1 5.0 C[N+]1(C)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL257804 11810 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 436 7 1 1 5.0 C[N+]1(C)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
44422699 11746 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182272 11746 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL227378 11746 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
15050948 102344 0 None -3 4 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 513 7 3 7 1.8 NCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
CHEMBL305403 102344 0 None -3 4 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 513 7 3 7 1.8 NCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
44400762 70224 0 None 2 2 Rat 6.4 pKi = 6.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 396 5 2 3 2.3 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2005.02.036
CHEMBL194870 70224 0 None 2 2 Rat 6.4 pKi = 6.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 396 5 2 3 2.3 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2005.02.036
9998202 68824 0 None 2 2 Rat 7.4 pKi = 7.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL192485 68824 0 None 2 2 Rat 7.4 pKi = 7.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
4601 205020 29 None -1 17 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 205020 29 None -1 17 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 205020 29 None -1 17 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
71449148 79128 0 None -4 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 436 6 0 4 5.5 COc1ccc([S@@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2114064 79128 0 None -4 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 436 6 0 4 5.5 COc1ccc([S@@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
156014205 177717 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4635385 177717 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650957 177717 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
162645520 183046 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 1117 25 4 11 9.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4742721 183046 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 1117 25 4 11 9.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4802414 183046 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 1117 25 4 11 9.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
122194374 123490 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 367 7 0 4 3.8 COc1ccc(CCC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3629534 123490 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 367 7 0 4 3.8 COc1ccc(CCC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
71716836 86526 0 None -4 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 348 4 0 7 1.9 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3[N+](=O)[O-])C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323442 86526 0 None -4 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 348 4 0 7 1.9 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3[N+](=O)[O-])C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL308924 103311 0 None 2 2 Human 4.4 pKi = 4.4 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 268 4 1 5 1.0 CCO/C(O)=C1\CN2CC(CCC2CN(C)C)C1=O 10.1021/jm020572p
155552185 173489 0 None -67608 16 Human 4.4 pKi = 4.4 Binding
Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 173489 0 None -67608 16 Human 4.4 pKi = 4.4 Binding
Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
25067048 12227 0 None -29 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 646 13 2 2 8.1 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1185245 12227 0 None -29 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 646 13 2 2 8.1 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL402207 12227 0 None -29 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 646 13 2 2 8.1 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
21509921 103979 0 None -371 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103979 0 None -371 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
28417 39799 48 None -1 12 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 39799 48 None -1 12 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
191 399 92 None -37 28 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 399 92 None -37 28 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 399 92 None -37 28 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 399 92 None -37 28 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 399 92 None -37 28 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
3198 203802 73 None -10 34 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203802 73 None -10 34 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203802 73 None -10 34 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
43815 186337 58 None -5 24 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL1708 186337 58 None -5 24 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL490 186337 58 None -5 24 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
90666113 108857 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 744 18 6 9 7.5 Cc1cc(C)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c(-c2ccc(O)c(Cl)c2)c1 10.1039/C1MD00140J
CHEMBL3219045 108857 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 744 18 6 9 7.5 Cc1cc(C)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c(-c2ccc(O)c(Cl)c2)c1 10.1039/C1MD00140J
132947 3803 8 None -309 9 Human 7.4 pKi = 7.4 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/s0960-894x(01)00186-x
361 3803 8 None -309 9 Human 7.4 pKi = 7.4 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/s0960-894x(01)00186-x
CHEMBL265256 3803 8 None -309 9 Human 7.4 pKi = 7.4 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/s0960-894x(01)00186-x
155519740 169838 0 None -141 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 3 hrs by beta counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 3 hrs by beta counting method
ChEMBL 1125 29 4 14 9.6 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCNCC(=O)N1c2ncccc2NC(=O)c2cccnc21 10.1021/acs.jmedchem.8b01967
CHEMBL4448108 169838 0 None -141 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 3 hrs by beta counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 3 hrs by beta counting method
ChEMBL 1125 29 4 14 9.6 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCNCC(=O)N1c2ncccc2NC(=O)c2cccnc21 10.1021/acs.jmedchem.8b01967
21509921 103979 0 None -371 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103979 0 None -371 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
422063 194403 2 None -2 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 298 6 0 2 3.1 C[N+](C)(C)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377384 194403 2 None -2 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 298 6 0 2 3.1 C[N+](C)(C)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL560649 194403 2 None -2 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 298 6 0 2 3.1 C[N+](C)(C)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
44593619 186877 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493980 186877 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44400180 68666 0 None 1 2 Rat 7.4 pKi = 7.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 397 5 1 4 2.7 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2005.02.036
CHEMBL192337 68666 0 None 1 2 Rat 7.4 pKi = 7.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 397 5 1 4 2.7 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2005.02.036
44379281 57242 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 506 9 1 5 5.3 CCOC(=O)N(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/S0960-894X(97)00109-1
CHEMBL166385 57242 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 506 9 1 5 5.3 CCOC(=O)N(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/S0960-894X(97)00109-1
86720830 191562 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 490 8 2 7 3.6 Cn1nc(C(=O)O)cc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
CHEMBL5203937 191562 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 490 8 2 7 3.6 Cn1nc(C(=O)O)cc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
70683405 74126 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2021477 74126 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2027984 74126 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
155511112 168960 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 7 0 4 4.4 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4435123 168960 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 7 0 4 4.4 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
137630994 160593 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CC(C[N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4103375 160593 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CC(C[N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4117267 160593 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CC(C[N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
448537 159703 86 None -28 25 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159703 86 None -28 25 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
44437295 11788 0 None -4 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
CHEMBL1182472 11788 0 None -4 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
CHEMBL239866 11788 0 None -4 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
10262466 97892 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 208 2 0 3 0.3 O=C1CCON1CC#CCN1CCCC1 10.1016/j.bmc.2007.09.003
CHEMBL275104 97892 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 208 2 0 3 0.3 O=C1CCON1CC#CCN1CCCC1 10.1016/j.bmc.2007.09.003
44409769 76179 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.6 C[C@@H]1C[C@H]1c1nc(NC2CC2)cc(N2CCCCCC2)n1 10.1016/j.bmcl.2006.01.006
CHEMBL206087 76179 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.6 C[C@@H]1C[C@H]1c1nc(NC2CC2)cc(N2CCCCCC2)n1 10.1016/j.bmcl.2006.01.006
44409796 76403 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 2 4 4.4 Cc1c(NC2CCCCCC2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL206780 76403 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 2 4 4.4 Cc1c(NC2CCCCCC2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
44409965 76623 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 306 5 1 6 2.5 COc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
CHEMBL207098 76623 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 306 5 1 6 2.5 COc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
10030021 169312 8 None -50 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 532 10 1 4 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4440484 169312 8 None -50 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 532 10 1 4 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
145961495 160899 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4127373 160899 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
10982070 5096 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 392 2 0 6 3.7 COC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL105945 5096 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 392 2 0 6 3.7 COC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
10486393 141170 0 None -436 5 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL1202000 141170 0 None -436 5 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL385625 141170 0 None -436 5 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
24809738 11784 0 None -79 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 209 3 0 3 1.1 Cc1cc(OCC#CC[N+](C)(C)C)no1 10.1016/j.bmc.2007.09.003
CHEMBL1182466 11784 0 None -79 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 209 3 0 3 1.1 Cc1cc(OCC#CC[N+](C)(C)C)no1 10.1016/j.bmc.2007.09.003
CHEMBL239655 11784 0 None -79 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 209 3 0 3 1.1 Cc1cc(OCC#CC[N+](C)(C)C)no1 10.1016/j.bmc.2007.09.003
15157138 99164 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 345 9 0 3 4.8 CCN(CC)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL284137 99164 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 345 9 0 3 4.8 CCN(CC)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
44406406 133014 0 None 12 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 340 3 1 4 2.6 COC1(C#CC(O)(c2ccccn2)C2CCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL370862 133014 0 None 12 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 340 3 1 4 2.6 COC1(C#CC(O)(c2ccccn2)C2CCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
59291452 112279 0 None 1 3 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298590 112279 0 None 1 3 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305615 112279 0 None 1 3 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
71452754 79127 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00090a006
CHEMBL2114061 79127 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00090a006
44420821 83872 0 None 15 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 437 5 1 2 5.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CC2CCC(C1)N2Cc1ccccc1 10.1021/jm061159a
CHEMBL221400 83872 0 None 15 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 437 5 1 2 5.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CC2CCC(C1)N2Cc1ccccc1 10.1021/jm061159a
2286 3134 48 None -1 29 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3134 48 None -1 29 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3134 48 None -1 29 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3134 48 None -1 29 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3134 48 None -1 29 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
44593625 187547 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498358 187547 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539120 187547 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
9821459 198759 7 None 4 3 Human 8.4 pKi = 8.4 Binding
Binding affinity for human cloned Muscarinic M3 receptorsBinding affinity for human cloned Muscarinic M3 receptors
ChEMBL 384 7 2 3 4.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(99)00327-3
CHEMBL59836 198759 7 None 4 3 Human 8.4 pKi = 8.4 Binding
Binding affinity for human cloned Muscarinic M3 receptorsBinding affinity for human cloned Muscarinic M3 receptors
ChEMBL 384 7 2 3 4.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(99)00327-3
44431391 145888 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 352 6 1 5 2.3 CN(C)C1(CNCCC2CCOCC2)COc2ccc(F)cc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL392186 145888 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 352 6 1 5 2.3 CN(C)C1(CNCCC2CCOCC2)COc2ccc(F)cc2OC1 10.1016/j.bmcl.2006.11.058
16086003 80021 0 None 114 4 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL214642 80021 0 None 114 4 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
9821459 198759 7 None 4 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 384 7 2 3 4.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1021/jm0003135
CHEMBL59836 198759 7 None 4 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 384 7 2 3 4.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1021/jm0003135
4134 72341 10 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 342 8 1 3 3.0 CC[N+](C)(CC)CCOC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL1996652 72341 10 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 342 8 1 3 3.0 CC[N+](C)(CC)CCOC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2106570 72341 10 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 342 8 1 3 3.0 CC[N+](C)(CC)CCOC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
15108133 110813 0 None -3 2 Rat 8.4 pKi = 8.4 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 335 4 0 3 3.8 CN1CC2CC1C[C@@H](OC(=O)C(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL326640 110813 0 None -3 2 Rat 8.4 pKi = 8.4 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 335 4 0 3 3.8 CN1CC2CC1C[C@@H](OC(=O)C(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
90666119 108865 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 728 19 6 9 6.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@H]3C[C@@]3(COC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219052 108865 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 728 19 6 9 6.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@H]3C[C@@]3(COC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
16125680 136114 0 None 70 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 429 5 1 2 4.8 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
CHEMBL373994 136114 0 None 70 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 429 5 1 2 4.8 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
90666114 108859 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3cc(F)ccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219047 108859 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3cc(F)ccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
90666117 108863 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 744 20 6 9 7.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219050 108863 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 744 20 6 9 7.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
16125683 84227 0 None 36 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 431 5 1 2 5.5 Cc1cccc(CN2CCC(N3CC(c4ccccc4)(C4CCCCC4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL222403 84227 0 None 36 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 431 5 1 2 5.5 Cc1cccc(CN2CCC(N3CC(c4ccccc4)(C4CCCCC4)NC3=O)CC2)c1 10.1021/jm061159a
53326837 58237 0 None 7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 722 17 5 10 5.3 C[N+]1(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)[C@@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@H]12 10.1016/j.bmcl.2011.01.043
CHEMBL1683942 58237 0 None 7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 722 17 5 10 5.3 C[N+]1(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)[C@@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@H]12 10.1016/j.bmcl.2011.01.043
118719921 115274 0 None 1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 115274 0 None 1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
54580133 61487 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 654 19 5 7 7.7 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773265 61487 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 654 19 5 7 7.7 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
140844405 176068 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 9 1 3 5.1 O=C(OC1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4474694 176068 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 9 1 3 5.1 O=C(OC1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597973 176068 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 9 1 3 5.1 O=C(OC1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
90666111 108855 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 18 6 9 7.2 Cc1ccc(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c(-c2ccc(O)c(Cl)c2)c1 10.1039/C1MD00140J
CHEMBL3219043 108855 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 18 6 9 7.2 Cc1ccc(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c(-c2ccc(O)c(Cl)c2)c1 10.1039/C1MD00140J
53322411 58209 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 380 8 1 3 5.9 CCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683914 58209 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 380 8 1 3 5.9 CCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16125682 83873 0 None 239 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 465 5 1 2 5.0 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
CHEMBL221401 83873 0 None 239 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 465 5 1 2 5.0 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
16115943 11742 0 None -5 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1182205 11742 0 None -5 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL220393 11742 0 None -5 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
44431380 87557 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 318 5 1 4 2.9 CN(C)C1(CNCC2CCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234257 87557 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 318 5 1 4 2.9 CN(C)C1(CNCC2CCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
44406346 135627 0 None 6 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 361 4 1 3 3.2 COC1(C#CC(O)(Cc2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL373256 135627 0 None 6 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 361 4 1 3 3.2 COC1(C#CC(O)(Cc2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
6075 149575 36 None -3 16 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 149575 36 None -3 16 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
44430470 86377 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 316 4 0 5 2.9 COC1CN(c2nc(C3CC3)nc(N3CCCCCC3)c2C)C1 10.1016/j.bmcl.2007.03.047
CHEMBL232208 86377 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 316 4 0 5 2.9 COC1CN(c2nc(C3CC3)nc(N3CCCCCC3)c2C)C1 10.1016/j.bmcl.2007.03.047
44430457 150137 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 328 3 0 4 4.4 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
CHEMBL395571 150137 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 328 3 0 4 4.4 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
44409981 75883 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CCC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205840 75883 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CCC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
70681307 74107 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2021479 74107 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2027890 74107 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
137630891 160582 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CCC([N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4085451 160582 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CCC([N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4117201 160582 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CCC([N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
44437256 12290 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 282 4 0 4 2.8 C(#CCN1CCCC1)COc1cc(-c2ccccc2)on1 10.1016/j.bmc.2007.09.003
CHEMBL1185707 12290 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 282 4 0 4 2.8 C(#CCN1CCCC1)COc1cc(-c2ccccc2)on1 10.1016/j.bmc.2007.09.003
CHEMBL428916 12290 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 282 4 0 4 2.8 C(#CCN1CCCC1)COc1cc(-c2ccccc2)on1 10.1016/j.bmc.2007.09.003
15050946 102173 0 None -1 4 Rat 5.4 pKi = 5.4 Binding
Compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to mmuscarinic acetylcholine receptor M3 of transfected rat A9L cellsCompound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to mmuscarinic acetylcholine receptor M3 of transfected rat A9L cells
ChEMBL 484 5 2 6 2.5 CNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
CHEMBL304391 102173 0 None -1 4 Rat 5.4 pKi = 5.4 Binding
Compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to mmuscarinic acetylcholine receptor M3 of transfected rat A9L cellsCompound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to mmuscarinic acetylcholine receptor M3 of transfected rat A9L cells
ChEMBL 484 5 2 6 2.5 CNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
15730 70774 73 None -1 10 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
CHEMBL195437 70774 73 None -1 10 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
122194377 123491 0 None 1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 412 8 1 5 3.6 COc1ccc(CCNC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
CHEMBL3629536 123491 0 None 1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 412 8 1 5 3.6 COc1ccc(CCNC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
71452382 83380 0 None -12 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205812 83380 0 None -12 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
11079969 163305 0 None -26 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 404 4 1 5 4.3 C=CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL420662 163305 0 None -26 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 404 4 1 5 4.3 C=CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
71575027 85796 0 None -8 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 379 8 0 4 4.4 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL2312389 85796 0 None -8 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 379 8 0 4 4.4 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccc(OC)cc2)C1 10.1021/jm301774u
10066369 119752 0 None -67 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 119752 0 None -67 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
44448538 12313 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 339 6 1 2 3.1 C[N+]1(C)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1185855 12313 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 339 6 1 2 3.1 C[N+]1(C)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL436850 12313 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 339 6 1 2 3.1 C[N+]1(C)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
44274400 98481 0 None -1 5 Human 4.4 pKi = 4.4 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL279520 98481 0 None -1 5 Human 4.4 pKi = 4.4 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
46227487 14012 0 None 1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 216 2 0 2 1.7 CC1(C)OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198047 14012 0 None 1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 216 2 0 2 1.7 CC1(C)OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL593861 14012 0 None 1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 216 2 0 2 1.7 CC1(C)OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
137630667 160545 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 3 0 1 2.7 C[N+](C)(C)CCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4100938 160545 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 3 0 1 2.7 C[N+](C)(C)CCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116890 160545 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 3 0 1 2.7 C[N+](C)(C)CCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
140844418 175836 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.9 O=C(OC1C[N+]2(CCCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4576060 175836 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.9 O=C(OC1C[N+]2(CCCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596067 175836 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.9 O=C(OC1C[N+]2(CCCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
75356563 156415 20 None 1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 184 3 1 4 1.0 c1csc(COC2CCNC2)n1 10.1021/acs.jmedchem.7b01113
CHEMBL4072787 156415 20 None 1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 184 3 1 4 1.0 c1csc(COC2CCNC2)n1 10.1021/acs.jmedchem.7b01113
631645 164324 1 None -1 3 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 565 9 3 8 2.4 CC(C)(C)OC(=O)NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL422053 164324 1 None -1 3 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 565 9 3 8 2.4 CC(C)(C)OC(=O)NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
44593622 187213 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL495888 187213 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL556390 187213 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
145960427 160903 0 None -3 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4127428 160903 0 None -3 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
16125623 137596 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 436 5 1 3 4.5 N#Cc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL376636 137596 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 436 5 1 3 4.5 N#Cc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
10026270 93681 0 None 18 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 440 6 2 3 4.5 O=C(N[C@H]1[C@@H]2CN(Cc3ccc4ccccc4c3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL249206 93681 0 None 18 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 440 6 2 3 4.5 O=C(N[C@H]1[C@@H]2CN(Cc3ccc4ccccc4c3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
140844397 176024 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.7 O=C(OC1C[N+]2(CCCOCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4567385 176024 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.7 O=C(OC1C[N+]2(CCCOCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597612 176024 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.7 O=C(OC1C[N+]2(CCCOCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
44593618 186876 0 None -4 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493979 186876 0 None -4 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
155528419 170762 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 6 0 4 4.0 COc1ccc(CCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4461216 170762 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 6 0 4 4.0 COc1ccc(CCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
137639541 156162 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 3 0 3 1.7 CN1CCCC(OCc2cccnc2)C1 10.1021/acs.jmedchem.7b01113
CHEMBL4070061 156162 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 3 0 3 1.7 CN1CCCC(OCc2cccnc2)C1 10.1021/acs.jmedchem.7b01113
10963509 18310 1 None -48 5 Human 6.4 pKi = 6.4 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 687 17 0 6 8.6 COc1ccccc1CN1CCC(C2CCN(CCCCCCCCN3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
CHEMBL127273 18310 1 None -48 5 Human 6.4 pKi = 6.4 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 687 17 0 6 8.6 COc1ccccc1CN1CCC(C2CCN(CCCCCCCCN3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
71454526 79049 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@@H]1C[C@@H]2C[C@H](C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL2113669 79049 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@@H]1C[C@@H]2C[C@H](C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
10344314 93679 0 None 12 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 462 8 2 5 3.1 COC(=O)c1ccc(CCN2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1 10.1016/j.bmcl.2007.06.081
CHEMBL249204 93679 0 None 12 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 462 8 2 5 3.1 COC(=O)c1ccc(CCN2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1 10.1016/j.bmcl.2007.06.081
10365534 154421 0 None 18 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 432 7 2 3 4.0 Cc1ccc(CCN2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1C 10.1016/j.bmcl.2007.06.081
CHEMBL401154 154421 0 None 18 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 432 7 2 3 4.0 Cc1ccc(CCN2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1C 10.1016/j.bmcl.2007.06.081
156015971 177707 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4648444 177707 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650880 177707 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
145961161 161058 0 None -4 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4129580 161058 0 None -4 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
10092649 192471 51 None -38 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1021/jm100697g
CHEMBL522460 192471 51 None -38 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1021/jm100697g
2230 461 55 None -588 10 Human 4.4 pKi = 4.4 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
296 461 55 None -588 10 Human 4.4 pKi = 4.4 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
CHEMBL7303 461 55 None -588 10 Human 4.4 pKi = 4.4 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
DB04365 461 55 None -588 10 Human 4.4 pKi = 4.4 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
137628858 160424 0 None -1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 CCOc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4074319 160424 0 None -1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 CCOc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115967 160424 0 None -1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 CCOc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
155510347 174139 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 398 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CCCN(C)C2)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4559952 174139 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 398 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CCCN(C)C2)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
2551 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
298 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
488 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
CHEMBL965 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
DB00411 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
162353388 180397 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC[C@H]1CO 10.1016/j.bmcl.2020.127632
CHEMBL4758633 180397 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC[C@H]1CO 10.1016/j.bmcl.2020.127632
44448457 11808 0 None -3 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 566 15 2 2 6.6 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1182638 11808 0 None -3 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 566 15 2 2 6.6 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL257586 11808 0 None -3 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 566 15 2 2 6.6 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
2551 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
298 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
488 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
CHEMBL965 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
DB00411 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
2551 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
298 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
488 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
CHEMBL965 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
DB00411 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
7022778 172214 10 None 1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@@H]2CCCN2)c1 10.1021/jm800145d
CHEMBL451335 172214 10 None 1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@@H]2CCCN2)c1 10.1021/jm800145d
2551 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
298 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
488 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
CHEMBL965 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
DB00411 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
2551 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
298 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
488 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
CHEMBL965 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
DB00411 782 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
1548953 205945 24 None -2 17 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 205945 24 None -2 17 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
2726 906 64 None -18 72 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 906 64 None -18 72 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 906 64 None -18 72 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 906 64 None -18 72 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 906 64 None -18 72 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
155556290 175882 0 None -257 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4554682 175882 0 None -257 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596434 175882 0 None -257 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
70687661 74104 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2021476 74104 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2027845 74104 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
118719924 115278 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 649 20 0 7 8.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354071 115278 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 649 20 0 7 8.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
11610557 71687 0 None -8 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1CC(O)c2ccccc2C1c1ccccc1 10.1021/jm050099q
CHEMBL197588 71687 0 None -8 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1CC(O)c2ccccc2C1c1ccccc1 10.1021/jm050099q
15050935 202272 0 None -1 2 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 381 3 2 6 1.1 CN1CCN(CC(=O)N2c3cc(CO)ccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL69423 202272 0 None -1 2 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 381 3 2 6 1.1 CN1CCN(CC(=O)N2c3cc(CO)ccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
156014875 177666 0 None -3 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4640846 177666 0 None -3 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650577 177666 0 None -3 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
162657652 180403 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 335 4 1 3 4.2 CCn1c2ccccc2c2ccc(NCC(=O)N3CCCCC3)cc21 10.1016/j.bmcl.2020.127632
CHEMBL4758742 180403 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 335 4 1 3 4.2 CCn1c2ccccc2c2ccc(NCC(=O)N3CCCCC3)cc21 10.1016/j.bmcl.2020.127632
24894631 176190 3 None -1 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCCC1c1ccco1 10.1021/jm800145d
CHEMBL460470 176190 3 None -1 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCCC1c1ccco1 10.1021/jm800145d
46227411 14006 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL1198027 14006 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL593443 14006 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
2551 782 23 None -54 11 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44318736 106538 0 None -3 4 Human 6.4 pKi = 6.4 Binding
The binding affinity was measured as inhibition of binding of [3H]- quinuclidinyl benzilate to m3 Muscarinic acetylcholine receptor M3 in membranes of CHO cellsThe binding affinity was measured as inhibition of binding of [3H]- quinuclidinyl benzilate to m3 Muscarinic acetylcholine receptor M3 in membranes of CHO cells
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
CHEMBL315428 106538 0 None -3 4 Human 6.4 pKi = 6.4 Binding
The binding affinity was measured as inhibition of binding of [3H]- quinuclidinyl benzilate to m3 Muscarinic acetylcholine receptor M3 in membranes of CHO cellsThe binding affinity was measured as inhibition of binding of [3H]- quinuclidinyl benzilate to m3 Muscarinic acetylcholine receptor M3 in membranes of CHO cells
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
19716 9177 5 None - 1 Rat 5.4 pKi = 5.4 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 194 2 0 2 0.6 CC(=O)N(C)CC#CCN1CCCC1 10.1021/jm00164a044
CHEMBL11081 9177 5 None - 1 Rat 5.4 pKi = 5.4 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 194 2 0 2 0.6 CC(=O)N(C)CC#CCN1CCCC1 10.1021/jm00164a044
10114698 4764 0 None -41 5 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 448 7 1 5 5.5 CCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL104210 4764 0 None -41 5 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 448 7 1 5 5.5 CCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
133640439 180791 1 None -7 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 1.9 O=C(O)C1CCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4763304 180791 1 None -7 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 1.9 O=C(O)C1CCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
44274433 99050 0 None -2 5 Human 4.3 pKi = 4.3 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL283320 99050 0 None -2 5 Human 4.3 pKi = 4.3 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
10851461 58203 35 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 296 3 2 3 3.7 O=C(Nc1ccccc1-c1ccccc1)OC1CCNCC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683908 58203 35 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 296 3 2 3 3.7 O=C(Nc1ccccc1-c1ccccc1)OC1CCNCC1 10.1016/j.bmcl.2011.01.043
15050953 101869 0 None -2 4 Rat 7.3 pKi = 7.3 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 536 9 2 7 4.0 CC(C)(C)OC(=O)NCCCCCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL303684 101869 0 None -2 4 Rat 7.3 pKi = 7.3 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 536 9 2 7 4.0 CC(C)(C)OC(=O)NCCCCCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
9985181 119852 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 556 9 1 4 6.1 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1)C(=O)c1ccc(F)cc1 10.1016/S0960-894X(97)00109-1
CHEMBL353140 119852 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 556 9 1 4 6.1 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1)C(=O)c1ccc(F)cc1 10.1016/S0960-894X(97)00109-1
122194373 123489 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 397 8 0 5 3.8 COc1ccc(CCC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
CHEMBL3629533 123489 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 397 8 0 5 3.8 COc1ccc(CCC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
2551 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
73355415 92101 0 None -2 13 Human 6.3 pKi = 6.3 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
CHEMBL2432039 92101 0 None -2 13 Human 6.3 pKi = 6.3 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
44593617 186848 0 None -3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493795 186848 0 None -3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
14939893 9443 0 None -112 5 Rat 6.3 pKi = 6.3 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL112244 9443 0 None -112 5 Rat 6.3 pKi = 6.3 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
44337638 110077 0 None -1 2 Rat 4.3 pKi = 4.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL325322 110077 0 None -1 2 Rat 4.3 pKi = 4.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
137642607 157972 0 None -2398 8 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091231 157972 0 None -2398 8 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
156016047 177685 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4647816 177685 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650722 177685 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
46227481 14024 0 None 1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198081 14024 0 None 1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL595022 14024 0 None 1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
1530 2151 44 None -57 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2151 44 None -57 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2151 44 None -57 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2151 44 None -57 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2151 44 None -57 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
2551 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44309151 201889 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 6 2 3 3.3 NCCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL66820 201889 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 6 2 3 3.3 NCCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
2200 3082 38 None -15 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
328 3082 38 None -15 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
4848 3082 38 None -15 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
CHEMBL9967 3082 38 None -15 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
DB00670 3082 38 None -15 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
187 253 34 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 253 34 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 253 34 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 253 34 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 253 34 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 253 34 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
137629744 160628 0 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1ccccc1CC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL4071109 160628 0 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1ccccc1CC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL4117602 160628 0 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1ccccc1CC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
44437298 11782 0 None -21 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 237 2 0 3 1.4 C[N+]1(CC#CCOC2=NOCC2)CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL1182460 11782 0 None -21 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 237 2 0 3 1.4 C[N+]1(CC#CCOC2=NOCC2)CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL239436 11782 0 None -21 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 237 2 0 3 1.4 C[N+]1(CC#CCOC2=NOCC2)CCCCC1 10.1016/j.bmc.2007.09.003
71452791 79241 0 None -21 2 Rat 4.3 pKi = 4.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)O[C@@H]1CC2CC1N(Cc1ccccc1)C2 10.1021/jm00090a006
CHEMBL2115123 79241 0 None -21 2 Rat 4.3 pKi = 4.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)O[C@@H]1CC2CC1N(Cc1ccccc1)C2 10.1021/jm00090a006
3652 45983 62 None -1 9 Human 5.3 pKi = 5.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 10.1038/s41586-020-2286-9
CHEMBL1535 45983 62 None -1 9 Human 5.3 pKi = 5.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 10.1038/s41586-020-2286-9
53325043 58214 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 450 13 1 3 7.9 CCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683919 58214 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 450 13 1 3 7.9 CCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16086039 12234 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 N[C@H]1CCCC[C@@H]1NC(=O)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL1185290 12234 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 N[C@H]1CCCC[C@@H]1NC(=O)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL405117 12234 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 N[C@H]1CCCC[C@@H]1NC(=O)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
155550632 175955 0 None -776 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 845 22 8 10 1.9 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4540949 175955 0 None -776 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 845 22 8 10 1.9 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597071 175955 0 None -776 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 845 22 8 10 1.9 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
70685504 74105 0 None -14 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)[C@H]1CCCC[C@H]1N(C)C 10.1016/j.bmc.2008.06.025
CHEMBL2021478 74105 0 None -14 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)[C@H]1CCCC[C@H]1N(C)C 10.1016/j.bmc.2008.06.025
CHEMBL2027846 74105 0 None -14 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)[C@H]1CCCC[C@H]1N(C)C 10.1016/j.bmc.2008.06.025
23352285 96331 2 None -4 3 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 219 2 0 3 2.6 O=Cc1ccc(C2=CN3CCC2CC3)s1 10.1016/S0960-894X(01)80824-6
CHEMBL264747 96331 2 None -4 3 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 219 2 0 3 2.6 O=Cc1ccc(C2=CN3CCC2CC3)s1 10.1016/S0960-894X(01)80824-6
71575652 85771 0 None -9 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 381 5 0 4 3.6 CN1CCC(c2ccccc2F)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
CHEMBL2312352 85771 0 None -9 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 381 5 0 4 3.6 CN1CCC(c2ccccc2F)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
11759058 120336 0 None -1 5 Human 4.3 pKi = 4.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL355851 120336 0 None -1 5 Human 4.3 pKi = 4.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
11674313 65656 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 329 3 1 4 3.4 Fc1cccc(F)c1-n1nc(OC2CCNCC2)c2ccccc21 10.1021/jm2007535
CHEMBL1836644 65656 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 329 3 1 4 3.4 Fc1cccc(F)c1-n1nc(OC2CCNCC2)c2ccccc21 10.1021/jm2007535
16086017 12196 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL1184940 12196 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL379483 12196 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
6098192 200116 11 None -1 3 Rat 6.3 pKi = 6.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
CHEMBL606901 200116 11 None -1 3 Rat 6.3 pKi = 6.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
2551 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44337748 9305 0 None 1 2 Rat 5.3 pKi = 5.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL111529 9305 0 None 1 2 Rat 5.3 pKi = 5.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
59707195 108852 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(F)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219040 108852 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(F)c3)CC2)ccc1O 10.1039/C1MD00140J
16115801 12189 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL1184882 12189 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL375851 12189 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
72712474 105972 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 310 3 1 5 1.1 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3091669 105972 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 310 3 1 5 1.1 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3139993 105972 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 310 3 1 5 1.1 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
9809330 115499 0 None -39 5 Human 8.3 pKi = 8.3 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0301235
CHEMBL335542 115499 0 None -39 5 Human 8.3 pKi = 8.3 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0301235
168289650 190904 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 504 8 2 5 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)cc2F)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5193776 190904 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 504 8 2 5 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)cc2F)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
15888010 202149 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 3 2 3 2.3 NC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL68584 202149 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 3 2 3 2.3 NC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
53321086 58210 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 394 9 1 3 6.3 CCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683915 58210 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 394 9 1 3 6.3 CCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16115950 135859 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL373515 135859 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
2028 2931 77 None -1 11 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm050099q
359 2931 77 None -1 11 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm050099q
4634 2931 77 None -1 11 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm050099q
CHEMBL1231 2931 77 None -1 11 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm050099q
DB01062 2931 77 None -1 11 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm050099q
10470 2453 5 None -11 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
1689 2453 5 None -11 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
4057 2453 5 None -11 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
CHEMBL524004 2453 5 None -11 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
DB04843 2453 5 None -11 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
44404147 168524 6 None -3 3 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1ccccc1 10.1021/jm050099q
CHEMBL439867 168524 6 None -3 3 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1ccccc1 10.1021/jm050099q
10646948 37649 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 4 3.8 O=C(NC1CCN(Cc2cccc(O)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL145913 37649 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 4 3.8 O=C(NC1CCN(Cc2cccc(O)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
180 397 50 None -23 38 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -23 38 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -23 38 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -23 38 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -23 38 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
5648 78002 7 None -1 5 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
CHEMBL2107687 78002 7 None -1 5 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
CHEMBL2111176 78002 7 None -1 5 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
44431388 86891 0 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 348 6 1 5 2.8 CN(C)C1(CNCCC2=CCSCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL233202 86891 0 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 348 6 1 5 2.8 CN(C)C1(CNCCC2=CCSCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
9883040 100071 0 None -14 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic M3 receptorBinding affinity towards human muscarinic M3 receptor
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL291339 100071 0 None -14 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic M3 receptorBinding affinity towards human muscarinic M3 receptor
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL542622 100071 0 None -14 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic M3 receptorBinding affinity towards human muscarinic M3 receptor
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
10025038 168261 0 None 26 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.3 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL437781 168261 0 None 26 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.3 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
11796509 40456 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 422 7 2 4 3.9 COc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)c1 10.1021/jm0003135
CHEMBL148450 40456 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 422 7 2 4 3.9 COc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)c1 10.1021/jm0003135
2381 656 43 None -9 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
374 656 43 None -9 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
7128 656 43 None -9 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL1101 656 43 None -9 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
DB00810 656 43 None -9 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
73345823 89385 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 305 10 0 3 4.1 CC[C@H](C)C(C(=O)OCCCN(CC)CC)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377392 89385 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 305 10 0 3 4.1 CC[C@H](C)C(C(=O)OCCCN(CC)CC)c1ccccc1 10.1016/j.bmc.2013.01.072
44400175 67427 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 307 5 1 2 4.2 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
CHEMBL190815 67427 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 307 5 1 2 4.2 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
44308910 202047 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 324 3 2 3 1.7 O=C(N1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL67814 202047 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 324 3 2 3 1.7 O=C(N1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
44406527 140118 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 CO[C@]1(C#CC(O)(c2cccnc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL381469 140118 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 CO[C@]1(C#CC(O)(c2cccnc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
53319786 58216 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 339 5 2 4 3.3 NCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683920 58216 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 339 5 2 4 3.3 NCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
155536739 171649 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 384 5 0 4 4.1 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
CHEMBL4473985 171649 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 384 5 0 4 4.1 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
44409651 76039 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 1 4 3.9 CCC1CCN(c2nc(C3CC3)nc(NC3CC3)c2C)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL205944 76039 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 1 4 3.9 CCC1CCN(c2nc(C3CC3)nc(NC3CC3)c2C)CC1 10.1016/j.bmcl.2006.01.006
10171570 76704 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 2 1 4 3.1 C1CCCN(c2nc(C3CC3)nc3c2CCCN3)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL207287 76704 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 2 1 4 3.1 C1CCCN(c2nc(C3CC3)nc3c2CCCN3)CC1 10.1016/j.bmcl.2006.01.006
44409463 140184 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 308 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(F)(F)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL381752 140184 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 308 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(F)(F)CC1 10.1016/j.bmcl.2006.01.006
10619926 39563 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 382 6 2 4 3.4 O=C(NC1CCN(Cc2ccoc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL147672 39563 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 382 6 2 4 3.4 O=C(NC1CCN(Cc2ccoc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
10316726 11923 0 None -40 5 Rat 7.3 pKi = 7.3 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
CHEMBL1183364 11923 0 None -40 5 Rat 7.3 pKi = 7.3 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
CHEMBL292857 11923 0 None -40 5 Rat 7.3 pKi = 7.3 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
16094783 136044 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL373888 136044 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
10951142 5151 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 496 6 0 6 5.9 CCOC(=O)c1c(CC)n(Cc2ccccc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106219 5151 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 496 6 0 6 5.9 CCOC(=O)c1c(CC)n(Cc2ccccc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
44430474 86576 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 290 3 0 4 2.9 FC1CN(c2cc(N3CCCCCC3)nc(C3CC3)n2)C1 10.1016/j.bmcl.2007.03.047
CHEMBL232417 86576 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 290 3 0 4 2.9 FC1CN(c2cc(N3CCCCCC3)nc(C3CC3)n2)C1 10.1016/j.bmcl.2007.03.047
44409461 74426 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 302 5 2 5 2.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(CO)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL203124 74426 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 302 5 2 5 2.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(CO)CC1 10.1016/j.bmcl.2006.01.006
44409556 75668 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 288 4 2 5 2.2 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(O)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL205582 75668 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 288 4 2 5 2.2 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(O)CC1 10.1016/j.bmcl.2006.01.006
44409963 76963 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 336 5 1 4 4.3 Cc1c(NC2CC2)nc(Cc2ccccc2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL208300 76963 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 336 5 1 4 4.3 Cc1c(NC2CC2)nc(Cc2ccccc2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
10925451 58464 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2ccc(Cl)cc21)c1ccccn1 10.1021/jm020895l
CHEMBL168707 58464 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2ccc(Cl)cc21)c1ccccn1 10.1021/jm020895l
11120347 120217 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
CHEMBL354841 120217 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
137655636 158190 0 None -234 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4093527 158190 0 None -234 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
44299635 100103 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL291562 100103 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
155543345 176112 0 None -537 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4543584 176112 0 None -537 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4598362 176112 0 None -537 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
6604789 100578 3 None -199 10 Human 4.3 pKi = 4.3 Binding
Binding affinity against Muscarinic M3 receptorBinding affinity against Muscarinic M3 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
CHEMBL294649 100578 3 None -199 10 Human 4.3 pKi = 4.3 Binding
Binding affinity against Muscarinic M3 receptorBinding affinity against Muscarinic M3 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
16125533 84233 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 400 7 1 1 4.2 C[N+](C)(CCN1CC(c2ccccc2)(c2ccccc2)NC1=O)Cc1ccccc1 10.1021/jm061160+
CHEMBL222426 84233 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 400 7 1 1 4.2 C[N+](C)(CCN1CC(c2ccccc2)(c2ccccc2)NC1=O)Cc1ccccc1 10.1021/jm061160+
44593623 187297 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496503 187297 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539373 187297 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
2551 782 23 None -346 11 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
298 782 23 None -346 11 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
488 782 23 None -346 11 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL965 782 23 None -346 11 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB00411 782 23 None -346 11 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
56963799 74546 0 None -1288 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to human recombinant M3 receptorBinding affinity to human recombinant M3 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031737 74546 0 None -1288 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to human recombinant M3 receptorBinding affinity to human recombinant M3 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
44627958 13922 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197374 13922 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569089 13922 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
44593616 192611 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL523518 192611 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
10916286 5033 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(Cl)c2C1O3 10.1021/jm011116o
CHEMBL105593 5033 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(Cl)c2C1O3 10.1021/jm011116o
137645406 157360 0 None -64 13 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4084262 157360 0 None -64 13 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
3055 1405 43 None -1 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
313 1405 43 None -1 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
7163 1405 43 None -1 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
CHEMBL936 1405 43 None -1 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
DB01231 1405 43 None -1 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
14537188 136023 0 None -16 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 341 8 1 4 3.6 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccc(O)cc1 10.1016/j.bmc.2013.01.072
CHEMBL37372 136023 0 None -16 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 341 8 1 4 3.6 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccc(O)cc1 10.1016/j.bmc.2013.01.072
9978073 93634 0 None 7 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 396 6 2 4 3.4 O=C(N[C@H]1[C@@H]2CN(Cc3cccs3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL249005 93634 0 None 7 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 396 6 2 4 3.4 O=C(N[C@H]1[C@@H]2CN(Cc3cccs3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
154734599 2467 8 None -19 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
327 2467 8 None -19 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
4108 2467 8 None -19 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
CHEMBL27673 2467 8 None -19 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
162353390 180367 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.1 O=C(CCN1CCCc2ccccc21)N1CCCC(CO)C1 10.1016/j.bmcl.2020.127632
CHEMBL4758316 180367 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.1 O=C(CCN1CCCc2ccccc21)N1CCCC(CO)C1 10.1016/j.bmcl.2020.127632
44448385 11805 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 406 7 1 3 4.8 CN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182633 11805 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 406 7 1 3 4.8 CN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL257174 11805 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 406 7 1 3 4.8 CN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
162353377 180583 0 None -14 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 CC1CCc2ccccc2N1CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4760904 180583 0 None -14 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 CC1CCc2ccccc2N1CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
24894514 172165 3 None -1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@H]1c1ccco1 10.1021/jm800145d
CHEMBL450729 172165 3 None -1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@H]1c1ccco1 10.1021/jm800145d
122194369 123485 0 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 383 7 0 5 3.5 COc1ccc(CCOC(=O)C2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
CHEMBL3629529 123485 0 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 383 7 0 5 3.5 COc1ccc(CCOC(=O)C2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
16125679 84595 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 479 5 1 2 5.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(C(F)(F)F)c2)CC1 10.1021/jm061159a
CHEMBL223925 84595 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 479 5 1 2 5.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(C(F)(F)F)c2)CC1 10.1021/jm061159a
44437270 12222 0 None -13 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL1185211 12222 0 None -13 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL398043 12222 0 None -13 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
155551903 175883 0 None -67 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 462 8 2 4 4.3 CCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4569929 175883 0 None -67 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 462 8 2 4 4.3 CCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596435 175883 0 None -67 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 462 8 2 4 4.3 CCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
162353378 182329 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC(O)C1 10.1016/j.bmcl.2020.127632
CHEMBL4792360 182329 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC(O)C1 10.1016/j.bmcl.2020.127632
16125593 84317 0 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 467 8 1 3 4.1 N#CC[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222916 84317 0 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 467 8 1 3 4.1 N#CC[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
2551 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
71450550 83393 0 None -1 16 Human 6.3 pKi = 6.3 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 83393 0 None -1 16 Human 6.3 pKi = 6.3 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
1210 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
1213 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
2725 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
33036 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
4411 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
616 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
6976 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
716121 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
90475904 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 905 45 None -79 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
155528270 175817 0 None -457 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4461081 175817 0 None -457 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595943 175817 0 None -457 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
44448500 12228 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 549 12 2 3 6.2 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1185248 12228 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 549 12 2 3 6.2 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL402282 12228 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 549 12 2 3 6.2 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
162658421 180519 0 None -11 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 CC1CCCC(C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4760150 180519 0 None -11 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 CC1CCCC(C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
53326338 58205 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 324 4 1 3 4.4 CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683910 58205 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 324 4 1 3 4.4 CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
10104167 2028 1 None -60 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/acs.jmedchem.7b01113
6937 2028 1 None -60 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL3121473 2028 1 None -60 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/acs.jmedchem.7b01113
155516845 169542 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 364 6 0 3 4.4 O=C(OCCCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4443613 169542 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 364 6 0 3 4.4 O=C(OCCCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
2551 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44437303 12220 1 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 271 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc21 10.1016/j.bmc.2007.09.003
CHEMBL1185162 12220 1 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 271 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc21 10.1016/j.bmc.2007.09.003
CHEMBL394329 12220 1 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 271 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc21 10.1016/j.bmc.2007.09.003
44431372 86887 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 368 7 1 4 3.7 CC(C)c1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 10.1016/j.bmcl.2006.11.058
CHEMBL233198 86887 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 368 7 1 4 3.7 CC(C)c1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 10.1016/j.bmcl.2006.11.058
26987 936 29 None -56 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
6063 936 29 None -56 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
671 936 29 None -56 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
CHEMBL1626 936 29 None -56 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
DB00283 936 29 None -56 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
118719931 115285 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 669 18 0 4 8.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)CC1 10.1021/jm501173q
CHEMBL3354078 115285 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 669 18 0 4 8.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)CC1 10.1021/jm501173q
155525691 170464 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CCN(C)CC2)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4456775 170464 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CCN(C)CC2)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
2230 461 55 None -1348 10 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
296 461 55 None -1348 10 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
CHEMBL7303 461 55 None -1348 10 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
DB04365 461 55 None -1348 10 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
2230 461 55 None -588 10 Human 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
296 461 55 None -588 10 Human 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
CHEMBL7303 461 55 None -588 10 Human 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
DB04365 461 55 None -588 10 Human 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
10957754 58735 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CC(C1=C(CCCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL169401 58735 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CC(C1=C(CCCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
118719929 115283 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 442 15 1 3 6.0 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354076 115283 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 442 15 1 3 6.0 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCO)CC1 10.1021/jm501173q
10606253 156731 0 None -2290 5 Rat 5.2 pKi = 5.2 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1152 27 4 13 9.2 CN(CCCCCCCCN(C)C(=O)CCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL407678 156731 0 None -2290 5 Rat 5.2 pKi = 5.2 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1152 27 4 13 9.2 CN(CCCCCCCCN(C)C(=O)CCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
71454562 79244 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 436 6 0 4 5.5 COc1ccc([S@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2115126 79244 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 436 6 0 4 5.5 COc1ccc([S@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
10251468 93635 0 None 20 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.2 Cc1ccc(C(C)N2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1 10.1016/j.bmcl.2007.06.081
CHEMBL249006 93635 0 None 20 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.2 Cc1ccc(C(C)N2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1 10.1016/j.bmcl.2007.06.081
55005 104296 7 None -14 3 Rat 6.2 pKi = 6.2 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 208 2 0 2 1.0 CC(=O)N(C)C(C)C#CCN1CCCC1 10.1021/jm00164a044
CHEMBL310852 104296 7 None -14 3 Rat 6.2 pKi = 6.2 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 208 2 0 2 1.0 CC(=O)N(C)C(C)C#CCN1CCCC1 10.1021/jm00164a044
137630084 160498 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1C[N+](C)(C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4070055 160498 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1C[N+](C)(C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116507 160498 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1C[N+](C)(C)CC2 10.1021/acs.jmedchem.7b01113
137629673 160612 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 198 3 0 0 2.6 C[N+](C)(C)CCc1cccc(Cl)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4094819 160612 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 198 3 0 0 2.6 C[N+](C)(C)CCc1cccc(Cl)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4117396 160612 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 198 3 0 0 2.6 C[N+](C)(C)CCc1cccc(Cl)c1 10.1021/acs.jmedchem.7b01113
425249 89367 8 None -10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 355 8 1 4 3.6 CC(C)N(CCOC(=O)C(O)(c1ccccc1)c1ccccc1)C(C)C 10.1016/j.bmc.2013.01.072
CHEMBL2377261 89367 8 None -10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 355 8 1 4 3.6 CC(C)N(CCOC(=O)C(O)(c1ccccc1)c1ccccc1)C(C)C 10.1016/j.bmc.2013.01.072
155563428 174714 0 None -79 5 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M3 receptor (unknown origin)Inhibition of muscarinic M3 receptor (unknown origin)
ChEMBL 475 7 3 9 2.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4572905 174714 0 None -79 5 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M3 receptor (unknown origin)Inhibition of muscarinic M3 receptor (unknown origin)
ChEMBL 475 7 3 9 2.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
2551 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
9998202 68824 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Ki value for rat Muscarinic acetylcholine receptor M3Ki value for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL192485 68824 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Ki value for rat Muscarinic acetylcholine receptor M3Ki value for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
54586985 61484 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 583 15 5 7 5.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773262 61484 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 583 15 5 7 5.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
10647703 120455 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 461 6 3 4 3.8 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)cc1F 10.1021/jm0003135
CHEMBL356181 120455 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 461 6 3 4 3.8 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)cc1F 10.1021/jm0003135
10622033 42536 0 None 3 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 420 7 2 3 4.2 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1021/jm0003135
CHEMBL150219 42536 0 None 3 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 420 7 2 3 4.2 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1021/jm0003135
10193093 76099 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 298 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CC2CCC(C2)C1 10.1016/j.bmcl.2006.01.006
CHEMBL205976 76099 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 298 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CC2CCC(C2)C1 10.1016/j.bmcl.2006.01.006
CHEMBL5078006 212757 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
168291613 191436 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 476 8 2 6 4.5 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cc(C(=O)O)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5202045 191436 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 476 8 2 6 4.5 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cc(C(=O)O)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
118737353 118554 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.2 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426700 118554 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.2 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
16065136 67584 0 None 3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910847 67584 0 None 3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2ccccc2)C1 10.1021/jm200884j
10525412 41730 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1ccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)cc1 10.1021/jm0003135
CHEMBL149486 41730 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1ccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)cc1 10.1021/jm0003135
11968014 12649 4 None -5 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/jm301774u
CHEMBL1187846 12649 4 None -5 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/jm301774u
140844422 175867 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3cccc(Cl)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4452706 175867 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3cccc(Cl)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596309 175867 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3cccc(Cl)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
24846938 89371 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 339 8 1 5 3.4 CCN(CC)CCOC(=O)C(O)(c1cccs1)C1CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL2377267 89371 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 339 8 1 5 3.4 CCN(CC)CCOC(=O)C(O)(c1cccs1)C1CCCCC1 10.1016/j.bmc.2013.01.072
16124705 84206 0 None 77 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 451 5 1 2 5.8 O=C1NC(c2ccccc2)(C2CCCCC2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
CHEMBL222207 84206 0 None 77 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 451 5 1 2 5.8 O=C1NC(c2ccccc2)(C2CCCCC2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
138711334 176752 0 None 3 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 382 4 2 3 4.5 O=C(Nc1ccc(F)cc1-c1cc(F)c(F)c(F)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4637155 176752 0 None 3 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 382 4 2 3 4.5 O=C(Nc1ccc(F)cc1-c1cc(F)c(F)c(F)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
16125335 137630 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 454 6 1 2 4.3 C[N+]1(C[C@H]2O[C@@H]2c2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL376900 137630 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 454 6 1 2 4.3 C[N+]1(C[C@H]2O[C@@H]2c2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
11595794 135178 0 None -2 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 3 4.4 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1C1CCCCC1 10.1021/jm050099q
CHEMBL372983 135178 0 None -2 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 3 4.4 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1C1CCCCC1 10.1021/jm050099q
16125681 84344 0 None 141 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 481 5 1 2 5.6 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
CHEMBL223079 84344 0 None 141 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 481 5 1 2 5.6 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
16125585 84328 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 456 8 1 2 4.4 C[N+]1(CCOCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222976 84328 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 456 8 1 2 4.4 C[N+]1(CCOCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
10204457 202698 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 453 6 0 6 4.0 COc1ccc(S(=O)(=O)c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL71971 202698 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 453 6 0 6 4.0 COc1ccc(S(=O)(=O)c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
44431387 86890 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 350 6 1 5 2.9 CN(C)C1(CNCCC2CCSCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL233201 86890 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 350 6 1 5 2.9 CN(C)C1(CNCCC2CCSCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
44443724 93555 0 None 51 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.1 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL248614 93555 0 None 51 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.1 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCCCC1 10.1016/j.bmcl.2007.06.081
10670917 164512 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 3 4 3.7 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
CHEMBL422665 164512 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 3 4 3.7 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
5387 94438 24 None -4 6 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O 10.1021/jm00111a032
CHEMBL253978 94438 24 None -4 6 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O 10.1021/jm00111a032
44593626 187270 0 None -1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496306 187270 0 None -1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539121 187270 0 None -1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
155511167 168991 0 None 2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 432 6 0 3 5.7 O=C(OCCCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4435641 168991 0 None 2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 432 6 0 3 5.7 O=C(OCCCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
155565770 175051 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 410 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4580590 175051 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 410 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
162353380 181912 0 None -1 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 259 2 0 3 1.8 O=C(CN1CCCc2cnccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4786868 181912 0 None -1 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 259 2 0 3 1.8 O=C(CN1CCCc2cnccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
155560305 175679 0 None -257 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 801 19 5 9 2.8 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4568151 175679 0 None -257 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 801 19 5 9 2.8 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4594890 175679 0 None -257 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 801 19 5 9 2.8 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
57326233 76833 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042406 76833 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079010 76833 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
16125470 84232 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 426 5 1 1 4.8 C[N+]1(Cc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061160+
CHEMBL222425 84232 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 426 5 1 1 4.8 C[N+]1(Cc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061160+
145963288 161067 0 None -3 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4129723 161067 0 None -3 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
300 2474 13 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 10.1021/jm800145d
4141 2474 13 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 10.1021/jm800145d
CHEMBL92387 2474 13 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 10.1021/jm800145d
44274317 82959 0 None -2 5 Human 4.2 pKi = 4.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21937 82959 0 None -2 5 Human 4.2 pKi = 4.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
44446841 12232 0 None -2 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1185281 12232 0 None -2 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL404557 12232 0 None -2 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
101176697 168311 20 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1963 53 22 24 -4.3 CC(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NC(C)(C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CO)Cc1ccccc1)C(C)C)C(C)C 10.1021/jm061160+
16132042 168311 20 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1963 53 22 24 -4.3 CC(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NC(C)(C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CO)Cc1ccccc1)C(C)C)C(C)C 10.1021/jm061160+
CHEMBL438243 168311 20 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1963 53 22 24 -4.3 CC(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NC(C)(C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CO)Cc1ccccc1)C(C)C)C(C)C 10.1021/jm061160+
631644 202378 1 None -1 3 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 551 8 3 8 2.0 CC(C)(C)OC(=O)NCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL70133 202378 1 None -1 3 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 551 8 3 8 2.0 CC(C)(C)OC(=O)NCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
137631178 160657 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 COc1cccc(CCC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4081662 160657 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 COc1cccc(CCC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4117768 160657 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 COc1cccc(CCC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
2551 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
11595794 135178 0 None -2 3 Rat 7.2 pKi = 7.2 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 3 4.4 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1C1CCCCC1 10.1021/jm050099q
CHEMBL372983 135178 0 None -2 3 Rat 7.2 pKi = 7.2 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 3 4.4 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1C1CCCCC1 10.1021/jm050099q
44406572 72497 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 347 3 1 3 3.0 CO[C@@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200208 72497 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 347 3 1 3 3.0 CO[C@@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44409745 139594 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 4 1 4 3.3 c1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL380135 139594 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 4 1 4 3.3 c1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44409976 139943 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 330 6 2 4 4.1 Cc1c(NCc2c(F)cccc2F)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL380954 139943 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 330 6 2 4 4.1 Cc1c(NCc2c(F)cccc2F)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
122203596 155265 0 None -50 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 627 14 3 7 4.3 CCC(=O)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1016/j.ejmech.2021.113159
CHEMBL4059733 155265 0 None -50 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 627 14 3 7 4.3 CCC(=O)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1016/j.ejmech.2021.113159
CHEMBL4066481 155265 0 None -50 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 627 14 3 7 4.3 CCC(=O)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1016/j.ejmech.2021.113159
129989 447 41 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
8584 447 41 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
CHEMBL43383 447 41 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
162649253 183063 0 None -57 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 807 12 1 6 7.9 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
CHEMBL4748004 183063 0 None -57 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 807 12 1 6 7.9 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
CHEMBL4802611 183063 0 None -57 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 807 12 1 6 7.9 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
25025581 200311 0 None 1 8 Human 7.2 pKi = 7.2 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
CHEMBL608151 200311 0 None 1 8 Human 7.2 pKi = 7.2 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
1016 3690 75 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3690 75 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3690 75 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3690 75 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3690 75 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3690 75 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
11045444 58877 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL170088 58877 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
156009698 177761 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 872 16 2 5 11.0 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4634575 177761 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 872 16 2 5 11.0 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651200 177761 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 872 16 2 5 11.0 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
118719927 115281 0 None -6 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354074 115281 0 None -6 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
71459909 78205 0 None 3 2 Human 6.2 pKi = 6.2 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 444 5 0 3 6.4 O=C(c1cccs1)N(c1c(Cl)cccc1Cl)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL2112313 78205 0 None 3 2 Human 6.2 pKi = 6.2 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 444 5 0 3 6.4 O=C(c1cccs1)N(c1c(Cl)cccc1Cl)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
137629935 160473 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 160473 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 160473 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
2551 782 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
298 782 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
488 782 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
CHEMBL965 782 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
DB00411 782 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
155522355 175835 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4451030 175835 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4596065 175835 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
2551 782 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 782 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 782 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 782 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 782 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
44274417 98437 0 None -6 5 Human 4.2 pKi = 4.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL279225 98437 0 None -6 5 Human 4.2 pKi = 4.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
44339221 8637 0 None - 1 Rat 4.2 pKi = 4.2 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heartThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heart
ChEMBL 220 2 0 3 2.0 CCC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
CHEMBL109593 8637 0 None - 1 Rat 4.2 pKi = 4.2 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heartThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heart
ChEMBL 220 2 0 3 2.0 CCC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
44406342 71826 0 None 5 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 5 1 3 3.3 COC1(C#CC(O)(Cc2ccccc2)Cc2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL197973 71826 0 None 5 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 5 1 3 3.3 COC1(C#CC(O)(Cc2ccccc2)Cc2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44430469 168143 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 5 2.4 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(=O)C1 10.1016/j.bmcl.2007.03.047
CHEMBL436814 168143 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 5 2.4 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(=O)C1 10.1016/j.bmcl.2007.03.047
24962988 182030 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 324 5 1 3 3.7 CCOC(=O)N(Cc1ccccc1-c1ccccc1)[C@H]1CCNC1 10.1016/j.bmcl.2008.06.071
CHEMBL478834 182030 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 324 5 1 3 3.7 CCOC(=O)N(Cc1ccccc1-c1ccccc1)[C@H]1CCNC1 10.1016/j.bmcl.2008.06.071
122194370 123487 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 353 6 0 4 3.4 COc1ccc(CCOC(=O)C2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3629530 123487 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 353 6 0 4 3.4 COc1ccc(CCOC(=O)C2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
132947 3803 8 None -999 9 Rat 6.2 pKi = 6.2 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00075a032
361 3803 8 None -999 9 Rat 6.2 pKi = 6.2 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00075a032
CHEMBL265256 3803 8 None -999 9 Rat 6.2 pKi = 6.2 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00075a032
164617895 187940 0 None -3467 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 24 10 13 -0.5 CC(=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CCCN)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4852868 187940 0 None -3467 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 24 10 13 -0.5 CC(=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CCCN)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028466 187940 0 None -3467 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 24 10 13 -0.5 CC(=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CCCN)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
155560013 175726 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4564922 175726 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595198 175726 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
132947 3803 8 None -999 9 Rat 6.2 pKi = 6.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00046a021
361 3803 8 None -999 9 Rat 6.2 pKi = 6.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00046a021
CHEMBL265256 3803 8 None -999 9 Rat 6.2 pKi = 6.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00046a021
44309107 101705 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 360 5 3 3 3.4 NCc1ccc(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)cc1 10.1016/s0960-894x(03)00350-0
CHEMBL302720 101705 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 360 5 3 3 3.4 NCc1ccc(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)cc1 10.1016/s0960-894x(03)00350-0
2551 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
24841480 183317 0 None -33 20 Human 7.2 pKi = 7.2 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 183317 0 None -33 20 Human 7.2 pKi = 7.2 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
119357 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
3264 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
368 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
CHEMBL279453 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
119357 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
3264 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
368 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
CHEMBL279453 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
155516383 176099 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4443219 176099 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4598230 176099 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
44448606 11813 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 310 6 2 3 2.6 OC(CCCN1CCNCC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1182652 11813 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 310 6 2 3 2.6 OC(CCCN1CCNCC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL258385 11813 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 310 6 2 3 2.6 OC(CCCN1CCNCC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
71718048 86527 0 None 1 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 348 4 0 7 1.9 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3[N+](=O)[O-])C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323443 86527 0 None 1 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 348 4 0 7 1.9 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3[N+](=O)[O-])C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
137635734 155571 0 None -229 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4063176 155571 0 None -229 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
162667844 181951 0 None -3 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 Cc1ccc2c(c1)CCCN2CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4787283 181951 0 None -3 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 Cc1ccc2c(c1)CCCN2CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
46227555 14016 0 None -5 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL1198062 14016 0 None -5 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL594376 14016 0 None -5 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
134149168 147714 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to human M3 receptor expressed in CHO cells measured after 90 mins by radioligand binding assayBinding affinity to human M3 receptor expressed in CHO cells measured after 90 mins by radioligand binding assay
ChEMBL 297 2 0 2 3.6 CN1CC[C@H]2CC(=O)[C@H](Cc3ccccc3)[C@H]3CCC[C@@H]1[C@H]23 10.1016/j.bmcl.2016.10.065
CHEMBL3936289 147714 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to human M3 receptor expressed in CHO cells measured after 90 mins by radioligand binding assayBinding affinity to human M3 receptor expressed in CHO cells measured after 90 mins by radioligand binding assay
ChEMBL 297 2 0 2 3.6 CN1CC[C@H]2CC(=O)[C@H](Cc3ccccc3)[C@H]3CCC[C@@H]1[C@H]23 10.1016/j.bmcl.2016.10.065
4746 203183 29 None -1 4 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL1334033 203183 29 None -1 4 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL75880 203183 29 None -1 4 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
66561967 74355 0 None 1 7 Human 6.2 pKi = 6.2 Binding
Inhibition of M3 muscarinic receptorInhibition of M3 muscarinic receptor
ChEMBL 213 2 0 1 2.0 C1CC2CCC1N2CC12C3C4C5C3C1C5C42 10.1016/j.bmcl.2012.04.077
CHEMBL2030626 74355 0 None 1 7 Human 6.2 pKi = 6.2 Binding
Inhibition of M3 muscarinic receptorInhibition of M3 muscarinic receptor
ChEMBL 213 2 0 1 2.0 C1CC2CCC1N2CC12C3C4C5C3C1C5C42 10.1016/j.bmcl.2012.04.077
611107 202246 1 None -1 3 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 451 7 3 7 0.4 NCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL69287 202246 1 None -1 3 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 451 7 3 7 0.4 NCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
4189 205195 91 None -12 34 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205195 91 None -12 34 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205195 91 None -12 34 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
53325336 58217 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 353 6 2 4 3.7 NCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683921 58217 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 353 6 2 4 3.7 NCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
11013666 59120 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 354 6 0 2 5.2 CN(C)CCC1=C(C(c2ccccc2)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL171102 59120 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 354 6 0 2 5.2 CN(C)CCC1=C(C(c2ccccc2)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
156015153 177732 0 None -18 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1105 24 2 10 10.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4641714 177732 0 None -18 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1105 24 2 10 10.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651018 177732 0 None -18 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1105 24 2 10 10.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
44318929 106379 0 None -21 4 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
CHEMBL314493 106379 0 None -21 4 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
44299589 194723 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL56275 194723 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
9937474 169902 0 None -3388 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 551 6 1 5 5.3 Nc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4448933 169902 0 None -3388 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 551 6 1 5 5.3 Nc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1016/j.ejmech.2021.113159
11092603 4792 0 None -9 5 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 524 7 0 7 5.8 C=CCOC(=O)c1c(C)n(Cc2ccc(OC)cc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL104332 4792 0 None -9 5 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 524 7 0 7 5.8 C=CCOC(=O)c1c(C)n(Cc2ccc(OC)cc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
155522355 175835 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4451030 175835 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596065 175835 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
187 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
137644962 157947 0 None -338 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091058 157947 0 None -338 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
10418181 9495 1 None -2691 4 Rat 5.2 pKi = 5.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 873 26 3 10 8.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL112500 9495 1 None -2691 4 Rat 5.2 pKi = 5.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 873 26 3 10 8.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL1201995 9495 1 None -2691 4 Rat 5.2 pKi = 5.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 873 26 3 10 8.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
176 394 63 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
9815331 201417 1 None -263 8 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL64000 201417 1 None -263 8 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
9815331 201417 1 None -263 8 Rat 6.2 pKi = 6.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 201417 1 None -263 8 Rat 6.2 pKi = 6.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
9815331 201417 1 None -263 8 Human 6.2 pKi = 6.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 201417 1 None -263 8 Human 6.2 pKi = 6.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
187 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
2551 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
162645430 183045 0 None -26 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 860 15 2 7 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4744233 183045 0 None -26 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 860 15 2 7 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4802409 183045 0 None -26 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 860 15 2 7 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
155672 4968 5 None -7 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL105198 4968 5 None -7 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL56734 4968 5 None -7 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
137631026 160603 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 230 1 0 1 3.0 C[N+](C)(C)C1CCc2ccc3ccoc3c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL4093215 160603 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 230 1 0 1 3.0 C[N+](C)(C)C1CCc2ccc3ccoc3c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL4117321 160603 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 230 1 0 1 3.0 C[N+](C)(C)C1CCc2ccc3ccoc3c2C1 10.1021/acs.jmedchem.7b01113
44328347 205817 0 None -3 3 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 317 1 1 2 3.6 OC1(C2=CN3CCC2CC3)c2ccccc2CCc2ccccc21 10.1016/S0960-894X(01)80824-6
CHEMBL94772 205817 0 None -3 3 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 317 1 1 2 3.6 OC1(C2=CN3CCC2CC3)c2ccccc2CCc2ccccc21 10.1016/S0960-894X(01)80824-6
44593621 192694 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524061 192694 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
24894630 188382 0 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc(C2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL508347 188382 0 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc(C2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL555475 188382 0 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc(C2CCC[N+]2(C)C)o1 10.1021/jm800145d
44309231 168931 0 None -7 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 6 2 3 3.7 CCC1(CCN)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL443267 168931 0 None -7 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 6 2 3 3.7 CCC1(CCN)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
53322412 58211 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 408 10 1 3 6.7 CCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683916 58211 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 408 10 1 3 6.7 CCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
138710714 176512 0 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 406 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(Br)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4633165 176512 0 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 406 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(Br)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
2705 3781 59 None -1 10 Rat 8.2 pKi = 8.2 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.02.036
360 3781 59 None -1 10 Rat 8.2 pKi = 8.2 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.02.036
443879 3781 59 None -1 10 Rat 8.2 pKi = 8.2 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.02.036
CHEMBL1382 3781 59 None -1 10 Rat 8.2 pKi = 8.2 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.02.036
DB01036 3781 59 None -1 10 Rat 8.2 pKi = 8.2 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.02.036
44627746 13928 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197392 13928 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569760 13928 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
2683 102415 24 None 1 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102415 24 None 1 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102415 24 None 1 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
10484263 58235 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 639 16 6 6 6.5 O=C(Nc1ccccc1-c1ccccc1)NC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683940 58235 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 639 16 6 6 6.5 O=C(Nc1ccccc1-c1ccccc1)NC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
16125619 84299 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 427 5 2 3 4.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(O)c2)CC1 10.1021/jm061159a
CHEMBL222804 84299 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 427 5 2 3 4.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(O)c2)CC1 10.1021/jm061159a
16125398 84693 0 None 20 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CC[C@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL224783 84693 0 None 20 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CC[C@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
71128 96362 18 None -288 8 Human 8.1 pKi = 8.1 Binding
Antimuscarinic potency and subset specificity was characterised by inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00085a017
CHEMBL26505 96362 18 None -288 8 Human 8.1 pKi = 8.1 Binding
Antimuscarinic potency and subset specificity was characterised by inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00085a017
59145957 123471 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629358 123471 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
3652 4034 72 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 4034 72 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 4034 72 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 4034 72 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 4034 72 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
44627740 197080 0 None -6 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL583051 197080 0 None -6 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
134272503 175837 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 9 1 4 4.7 COc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
CHEMBL4545504 175837 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 9 1 4 4.7 COc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
CHEMBL4596068 175837 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 9 1 4 4.7 COc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
10646906 118728 0 None -2 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 3 4 3.7 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)cc1 10.1021/jm0003135
CHEMBL343449 118728 0 None -2 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 3 4 3.7 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)cc1 10.1021/jm0003135
44406321 72433 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 415 3 1 3 4.3 CO[C@]1(C#CC(O)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL199981 72433 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 415 3 1 3 4.3 CO[C@]1(C#CC(O)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406395 139750 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 3 1 3 3.7 CO[C@]1(C#CC(O)(c2cccc(C)c2)c2cccc(C)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL380583 139750 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 3 1 3 3.7 CO[C@]1(C#CC(O)(c2cccc(C)c2)c2cccc(C)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406689 140754 0 None 5 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 COC1(C#CC(O)(c2ccccc2)c2cccnn2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL383248 140754 0 None 5 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 COC1(C#CC(O)(c2ccccc2)c2cccnn2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
16125621 83945 0 None 22 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 426 5 2 3 4.2 Nc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL221829 83945 0 None 22 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 426 5 2 3 4.2 Nc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
44409751 74094 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CCC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL202729 74094 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CCC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44409945 139634 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(N[C@H]2C[C@@H]2C)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL380314 139634 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(N[C@H]2C[C@@H]2C)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL5069430 212446 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3cccnc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074216 212544 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
90200594 190087 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 477 8 2 7 3.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)O)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5181855 190087 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 477 8 2 7 3.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)O)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
134346261 190993 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 492 8 2 6 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2csc(C(=O)O)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5195224 190993 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 492 8 2 6 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2csc(C(=O)O)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
86720815 191461 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 486 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5202567 191461 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 486 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
86720819 191480 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 486 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)O)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5202787 191480 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 486 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)O)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
118737359 118561 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426707 118561 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
9913892 204122 0 None 100 2 Human 8.1 pKi = 8.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 499 6 0 5 5.7 O=C(c1ccc([N+](=O)[O-])s1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL83459 204122 0 None 100 2 Human 8.1 pKi = 8.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 499 6 0 5 5.7 O=C(c1ccc([N+](=O)[O-])s1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
155518181 169694 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 404 4 0 3 5.2 O=C(OCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4446039 169694 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 404 4 0 3 5.2 O=C(OCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
10203251 5153 0 None -35 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 434 5 0 6 4.8 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(OC)cc2CCN1C3 10.1021/jm011116o
CHEMBL106224 5153 0 None -35 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 434 5 0 6 4.8 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(OC)cc2CCN1C3 10.1021/jm011116o
9931930 108113 0 None -35 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 5 1 5 4.8 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL320465 108113 0 None -35 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 5 1 5 4.8 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
10770914 24857 0 None -239 5 Rat 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 691 25 3 7 6.4 CN(CCCCCCCCN(C)C(=O)CCCCCNCCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
CHEMBL134692 24857 0 None -239 5 Rat 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 691 25 3 7 6.4 CN(CCCCCCCCN(C)C(=O)CCCCCNCCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
9894173 14981 2 None -776 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 565 6 1 5 5.6 Cc1cccc(C(=O)N2CCC(N3CCC(Cc4ccc(S(=O)(=O)c5cccc(Cl)c5)cc4)CC3)CC2)c1N 10.1021/jm301774u
CHEMBL12098 14981 2 None -776 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 565 6 1 5 5.6 Cc1cccc(C(=O)N2CCC(N3CCC(Cc4ccc(S(=O)(=O)c5cccc(Cl)c5)cc4)CC3)CC2)c1N 10.1021/jm301774u
2551 782 23 None -54 11 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44377401 56248 1 None - 1 Rat 6.2 pKi = 6.2 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 293 9 1 3 1.8 CN(CC#CCN1CCCC1)C(=O)CCCCCCCN 10.1021/jm00164a044
CHEMBL1202134 56248 1 None - 1 Rat 6.2 pKi = 6.2 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 293 9 1 3 1.8 CN(CC#CCN1CCCC1)C(=O)CCCCCCCN 10.1021/jm00164a044
CHEMBL163875 56248 1 None - 1 Rat 6.2 pKi = 6.2 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 293 9 1 3 1.8 CN(CC#CCN1CCCC1)C(=O)CCCCCCCN 10.1021/jm00164a044
44207909 16520 1 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1242923 16520 1 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
10969390 59365 0 None -97 6 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 324 7 0 2 4.5 CC(C1=C(CCN(C)CCF)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL172233 59365 0 None -97 6 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 324 7 0 2 4.5 CC(C1=C(CCN(C)CCF)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
187 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
294 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
65 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
8593 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
CHEMBL667 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
DB03128 253 34 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
137636308 155661 0 None -22 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4064222 155661 0 None -22 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
44448530 12229 0 None 1 2 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 386 7 1 3 4.5 OC(CCCN1CCN(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185259 12229 0 None 1 2 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 386 7 1 3 4.5 OC(CCCN1CCN(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL403029 12229 0 None 1 2 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 386 7 1 3 4.5 OC(CCCN1CCN(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
44443734 93804 0 None 16 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)[C@@](O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL250031 93804 0 None 16 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)[C@@](O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
71720489 86531 0 None 1 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 303 3 0 5 2.0 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323447 86531 0 None 1 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 303 3 0 5 2.0 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
57326325 76831 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042554 76831 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078987 76831 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
57326325 76831 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL2042554 76831 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL2078987 76831 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
5318 15400 44 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15400 44 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15400 44 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
11498 2970 33 None -38 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
4995951 2970 33 None -38 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
CHEMBL59898 2970 33 None -38 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
44448421 12231 0 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185269 12231 0 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL403773 12231 0 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
162675053 182676 0 None -11 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 5 1 3 3.2 O=C(CCN1CCCc2ccccc21)NCc1cccs1 10.1016/j.bmcl.2020.127632
CHEMBL4796491 182676 0 None -11 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 5 1 3 3.2 O=C(CCN1CCCc2ccccc21)NCc1cccs1 10.1016/j.bmcl.2020.127632
156012563 177673 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4637485 177673 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650635 177673 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
156015045 177690 0 None -17 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4648218 177690 0 None -17 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650765 177690 0 None -17 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
44274432 79717 0 None -5 5 Human 4.1 pKi = 4.1 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21328 79717 0 None -5 5 Human 4.1 pKi = 4.1 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
16125529 136682 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL374987 136682 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
44437249 11767 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 235 3 0 3 1.6 Cc1cc(OCC#CC[N+]2(C)CCCC2)no1 10.1016/j.bmc.2007.09.003
CHEMBL1182436 11767 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 235 3 0 3 1.6 Cc1cc(OCC#CC[N+]2(C)CCCC2)no1 10.1016/j.bmc.2007.09.003
CHEMBL238825 11767 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 235 3 0 3 1.6 Cc1cc(OCC#CC[N+]2(C)CCCC2)no1 10.1016/j.bmc.2007.09.003
24882532 94674 0 None -5 5 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cells
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255523 94674 0 None -5 5 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cells
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
44318817 168548 0 None -32 4 Human 5.1 pKi = 5.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL440138 168548 0 None -32 4 Human 5.1 pKi = 5.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
11808947 59141 0 None -14 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 CC(C1=C(CN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL171216 59141 0 None -14 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 CC(C1=C(CN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
108993425 181176 1 None -19 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 O=C(CN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4777543 181176 1 None -19 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 O=C(CN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
44448575 11812 0 None 1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 3 3.0 CN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182650 11812 0 None 1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 3 3.0 CN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL258161 11812 0 None 1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 3 3.0 CN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
156015978 177748 0 None -35 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4636899 177748 0 None -35 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651111 177748 0 None -35 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL69452 202276 0 None -4 5 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 331 6 1 5 2.7 CCO/C(O)=C1\CN2CC(CCC2COCc2ccccc2)C1=O 10.1021/jm020572p
44318766 204037 0 None -5 4 Human 5.1 pKi = 5.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
CHEMBL82754 204037 0 None -5 4 Human 5.1 pKi = 5.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
137644950 157946 0 None -1 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 4 0 3 1.6 CN1CCC(COCc2cccnc2)C1 10.1021/acs.jmedchem.7b01113
CHEMBL4091032 157946 0 None -1 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 4 0 3 1.6 CN1CCC(COCc2cccnc2)C1 10.1021/acs.jmedchem.7b01113
164623076 187982 0 None -1995 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4872608 187982 0 None -1995 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028732 187982 0 None -1995 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
24865895 95559 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL259662 95559 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL390842 95559 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
44448496 11807 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 401 7 1 2 4.7 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182637 11807 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 401 7 1 2 4.7 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL257547 11807 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 401 7 1 2 4.7 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
44422692 11748 0 None -5 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182296 11748 0 None -5 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL228144 11748 0 None -5 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
24865895 95559 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL259662 95559 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL390842 95559 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
24865895 95559 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
CHEMBL259662 95559 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
CHEMBL390842 95559 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
44309135 96120 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 7 2 3 3.7 NCCCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL263040 96120 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 7 2 3 3.7 NCCCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
90666109 108851 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(O)cc(F)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219039 108851 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(O)cc(F)c3)CC2)ccc1O 10.1039/C1MD00140J
44247935 194902 0 None -234 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 294 5 0 3 4.1 C[C@@H](c1ccccn1)c1c(CCN(C)C)oc2ccccc12 10.1021/jm900933k
CHEMBL563920 194902 0 None -234 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 294 5 0 3 4.1 C[C@@H](c1ccccn1)c1c(CCN(C)C)oc2ccccc12 10.1021/jm900933k
1209 1628 69 None -30 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
203 1628 69 None -30 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
3386 1628 69 None -30 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
CHEMBL41 1628 69 None -30 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
DB00472 1628 69 None -30 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
2551 782 23 None -54 11 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
53317169 58206 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 338 5 1 3 4.8 CCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683911 58206 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 338 5 1 3 4.8 CCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
44593627 192696 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524071 192696 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL541671 192696 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
46905988 91930079 10318 0 None 3 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 8 2 3 3.7 O=C(N[C@H]1[C@@H]2CN(CCCc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL1162964 10318 0 None 3 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 8 2 3 3.7 O=C(N[C@H]1[C@@H]2CN(CCCc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
132712 171232 13 None -25 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL 567 10 1 5 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccc(Cl)cc3C(=O)Nc3cccnc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4468100 171232 13 None -25 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL 567 10 1 5 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccc(Cl)cc3C(=O)Nc3cccnc32)CC1 10.1021/acs.jmedchem.8b01967
155560140 175773 0 None -524 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4565234 175773 0 None -524 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595575 175773 0 None -524 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
36014865 182088 2 None -6 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 280 4 1 2 3.5 O=C(CCN1CCCc2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2020.127632
CHEMBL4789054 182088 2 None -6 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 280 4 1 2 3.5 O=C(CCN1CCCc2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2020.127632
71128 96362 18 None -288 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL26505 96362 18 None -288 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
137629935 160473 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 160473 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 160473 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
24894637 188133 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL504733 188133 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL553434 188133 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
46227459 14020 0 None 1 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL1198076 14020 0 None 1 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL594802 14020 0 None 1 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
611037 201999 1 None -1 4 Rat 7.1 pKi = 7.1 Binding
The compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M3 of transfected A9L cells.The compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M3 of transfected A9L cells.
ChEMBL 399 4 1 5 2.2 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCl)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL67532 201999 1 None -1 4 Rat 7.1 pKi = 7.1 Binding
The compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M3 of transfected A9L cells.The compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M3 of transfected A9L cells.
ChEMBL 399 4 1 5 2.2 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCl)CC2)c2ccccc21 10.1021/jm00111a032
118500 156457 57 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 165 4 1 2 1.5 CNCCc1cccc(OC)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4073256 156457 57 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 165 4 1 2 1.5 CNCCc1cccc(OC)c1 10.1021/acs.jmedchem.7b01113
137629935 160473 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 160473 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 160473 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
10381417 68326 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2C)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
CHEMBL192061 68326 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2C)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
44430472 86575 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 272 3 0 4 2.9 c1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
CHEMBL232416 86575 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 272 3 0 4 2.9 c1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
44430456 167840 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 314 3 0 4 4.0 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCCC1 10.1016/j.bmcl.2007.03.047
CHEMBL434765 167840 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 314 3 0 4 4.0 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCCC1 10.1016/j.bmcl.2007.03.047
44409937 75642 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 287 4 2 5 2.9 Nc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205482 75642 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 287 4 2 5 2.9 Nc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44409982 75894 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 314 4 1 4 4.4 Cc1c(NC2CC2)nc(C2CCCC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205841 75894 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 314 4 1 4 4.4 Cc1c(NC2CC2)nc(C2CCCC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
10236419 75921 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 290 4 1 5 2.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205853 75921 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 290 4 1 5 2.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
44409754 76351 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 284 4 1 4 3.4 C=C1CCN(c2nc(C3CC3)nc(NC3CC3)c2C)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL206480 76351 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 284 4 1 4 3.4 C=C1CCN(c2nc(C3CC3)nc(NC3CC3)c2C)CC1 10.1016/j.bmcl.2006.01.006
44409978 139661 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 314 7 2 5 4.0 Cc1c(NCCc2cccs2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL380477 139661 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 314 7 2 5 4.0 Cc1c(NCCc2cccs2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
44379080 57857 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 678 10 0 5 7.5 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3C(=O)N(C(=O)c3ccc(F)cc3)c3ccccc32)CC1)C(=O)c1ccc(F)cc1 10.1016/S0960-894X(97)00109-1
CHEMBL168149 57857 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 678 10 0 5 7.5 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3C(=O)N(C(=O)c3ccc(F)cc3)c3ccccc32)CC1)C(=O)c1ccc(F)cc1 10.1016/S0960-894X(97)00109-1
3652 4034 72 None -3 18 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
57 4034 72 None -3 18 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
60809 4034 72 None -3 18 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
CHEMBL21536 4034 72 None -3 18 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
DB15357 4034 72 None -3 18 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
9909908 13408 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
CHEMBL1193635 13408 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
CHEMBL545077 13408 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
11071537 26291 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 495 17 0 10 5.5 COc1nsnc1OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL136027 26291 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 495 17 0 10 5.5 COc1nsnc1OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
2396803 204406 4 None 10 2 Human 7.1 pKi = 7.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 398 7 0 2 5.3 O=C(CCc1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85950 204406 4 None 10 2 Human 7.1 pKi = 7.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 398 7 0 2 5.3 O=C(CCc1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
3652 4034 72 None -3 18 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4034 72 None -3 18 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4034 72 None -3 18 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4034 72 None -3 18 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4034 72 None -3 18 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
44409660 75583 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 362 6 1 4 4.7 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(Cc2ccccc2)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL205140 75583 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 362 6 1 4 4.7 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(Cc2ccccc2)CC1 10.1016/j.bmcl.2006.01.006
44430466 92869 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 311 3 0 5 3.0 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C#N)C1 10.1016/j.bmcl.2007.03.047
CHEMBL245137 92869 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 311 3 0 5 3.0 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C#N)C1 10.1016/j.bmcl.2007.03.047
44299564 197409 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL58824 197409 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
44318781 106495 0 None 5 2 Human 6.1 pKi = 6.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 415 6 0 4 4.9 O=C(c1ccc([N+](=O)[O-])cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL315127 106495 0 None 5 2 Human 6.1 pKi = 6.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 415 6 0 4 4.9 O=C(c1ccc([N+](=O)[O-])cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
14939894 10199 0 None -467 4 Rat 6.1 pKi = 6.1 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 742 28 3 8 8.0 COc1ccccc1CNCCCCCCN(C)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL116172 10199 0 None -467 4 Rat 6.1 pKi = 6.1 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 742 28 3 8 8.0 COc1ccccc1CNCCCCCCN(C)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
2736067 87102 67 None -93 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from recombinant muscarinic M3 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-NMS from recombinant muscarinic M3 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1cc(Cl)cc(N2CCNCC2)c1 10.1021/jm400140q
CHEMBL2335158 87102 67 None -93 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from recombinant muscarinic M3 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-NMS from recombinant muscarinic M3 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1cc(Cl)cc(N2CCNCC2)c1 10.1021/jm400140q
108993439 179280 1 None -3 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 CC1Cc2ccccc2N1CC(=O)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4745429 179280 1 None -3 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 CC1Cc2ccccc2N1CC(=O)N1CCCC1 10.1016/j.bmcl.2020.127632
44339221 8637 0 None - 1 Rat 4.1 pKi = 4.1 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary glandThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary gland
ChEMBL 220 2 0 3 2.0 CCC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
CHEMBL109593 8637 0 None - 1 Rat 4.1 pKi = 4.1 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary glandThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary gland
ChEMBL 220 2 0 3 2.0 CCC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
155562285 175269 0 None 1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4585326 175269 0 None 1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
26987 936 29 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 936 29 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 936 29 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 936 29 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 936 29 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
44308746 202153 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 3 2 3 2.6 CC1(N)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL68609 202153 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 3 2 3 2.6 CC1(N)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
90666110 108853 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)c(O)cc3F)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219041 108853 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)c(O)cc3F)CC2)ccc1O 10.1039/C1MD00140J
71452792 79243 0 None -1 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1[C@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00090a006
CHEMBL2115125 79243 0 None -1 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1[C@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00090a006
410345 89373 3 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 333 8 1 4 3.4 CCN(CC)CCOC(=O)C(c1ccccc1)C1(O)CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL2377269 89373 3 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 333 8 1 4 3.4 CCN(CC)CCOC(=O)C(c1ccccc1)C1(O)CCCCC1 10.1016/j.bmc.2013.01.072
16125571 84726 0 None 79 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL225074 84726 0 None 79 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
90666121 108867 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 742 18 6 9 7.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C3CCC2CC(OC(=O)Nc2ccccc2-c2ccc(O)c(Cl)c2)C3)ccc1O 10.1039/C1MD00140J
CHEMBL3219054 108867 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 742 18 6 9 7.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C3CCC2CC(OC(=O)Nc2ccccc2-c2ccc(O)c(Cl)c2)C3)ccc1O 10.1039/C1MD00140J
10718110 39675 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 2 4 3.8 Cc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1021/jm0003135
CHEMBL147778 39675 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 2 4 3.8 Cc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1021/jm0003135
44627852 13925 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 338 4 0 1 5.9 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197387 13925 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 338 4 0 1 5.9 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569712 13925 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 338 4 0 1 5.9 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
2335 11743 21 None -1 12 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
8478 11743 21 None -1 12 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL1182210 11743 21 None -1 12 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL221753 11743 21 None -1 12 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
134271233 175965 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 428 6 1 3 4.3 O=C(OC1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4591883 175965 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 428 6 1 3 4.3 O=C(OC1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597134 175965 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 428 6 1 3 4.3 O=C(OC1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
156015807 177724 0 None -63 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4641726 177724 0 None -63 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650973 177724 0 None -63 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
162677523 183092 0 None -104 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 930 14 2 10 5.8 CN(C)c1ccc2c(-c3ccc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
CHEMBL4756833 183092 0 None -104 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 930 14 2 10 5.8 CN(C)c1ccc2c(-c3ccc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
CHEMBL4802932 183092 0 None -104 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 930 14 2 10 5.8 CN(C)c1ccc2c(-c3ccc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
170332 160429 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 160429 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 160429 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
11001809 58772 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL169594 58772 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
11011332 120289 1 None -2 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL355560 120289 1 None -2 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
170332 160429 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 160429 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 160429 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
57326142 76827 0 None -4 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL2042401 76827 0 None -4 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL2078965 76827 0 None -4 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
24894515 176296 4 None -1 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@@H]1c1ccco1 10.1021/jm800145d
CHEMBL461502 176296 4 None -1 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@@H]1c1ccco1 10.1021/jm800145d
16125371 84335 0 None 28 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 5 1 2 4.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm061159a
CHEMBL223017 84335 0 None 28 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 5 1 2 4.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm061159a
44622849 195116 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of muscarinic receptor 3Inhibition of muscarinic receptor 3
ChEMBL 293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3 10.1016/j.bmcl.2009.07.063
CHEMBL565547 195116 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of muscarinic receptor 3Inhibition of muscarinic receptor 3
ChEMBL 293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3 10.1016/j.bmcl.2009.07.063
49783209 17427 0 None -1445 27 Human 6.1 pKi = 6.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17427 0 None -1445 27 Human 6.1 pKi = 6.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
135398745 2869 108 None -27 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2869 108 None -27 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2869 108 None -27 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2869 108 None -27 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
16125570 141784 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1ccccc1CN1CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061159a
CHEMBL388541 141784 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1ccccc1CN1CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061159a
9794266 156609 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 205 2 0 2 2.1 COc1cccc2c1CC(N(C)C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4075227 156609 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 205 2 0 2 2.1 COc1cccc2c1CC(N(C)C)CC2 10.1021/acs.jmedchem.7b01113
11184481 199743 12 None -2 4 Human 5.1 pKi = 5.1 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 258 1 0 5 1.8 Cc1ccc2oc(N3CCN4CCC3CC4)nc2n1 10.1021/jm9015075
CHEMBL604798 199743 12 None -2 4 Human 5.1 pKi = 5.1 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 258 1 0 5 1.8 Cc1ccc2oc(N3CCN4CCC3CC4)nc2n1 10.1021/jm9015075
71718668 86372 0 None 1 2 Rat 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 337 3 0 5 2.7 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3Cl)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2321893 86372 0 None 1 2 Rat 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 337 3 0 5 2.7 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3Cl)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
53325044 58218 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 367 7 2 4 4.1 NCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683922 58218 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 367 7 2 4 4.1 NCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
149706871 177063 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 358 5 2 4 4.0 COc1ccc(-c2cc(F)ccc2NC(=O)OCC2CCNCC2)cc1 10.1021/acs.jmedchem.0c00297
CHEMBL4641288 177063 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 358 5 2 4 4.0 COc1ccc(-c2cc(F)ccc2NC(=O)OCC2CCNCC2)cc1 10.1021/acs.jmedchem.0c00297
CHEMBL69452 202276 0 None -4 5 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 331 6 1 5 2.7 CCO/C(O)=C1\CN2CC(CCC2COCc2ccccc2)C1=O 10.1021/jm020572p
156015141 177692 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 668 11 1 4 8.2 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4642045 177692 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 668 11 1 4 8.2 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4650774 177692 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 668 11 1 4 8.2 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.9b02172
156015254 177712 0 None -19 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 984 19 2 7 10.6 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4649420 177712 0 None -19 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 984 19 2 7 10.6 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650938 177712 0 None -19 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 984 19 2 7 10.6 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
44627741 196005 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 317 4 0 2 5.2 CN1CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL571123 196005 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 317 4 0 2 5.2 CN1CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
162654942 183089 0 None -44 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 833 17 2 7 8.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4754371 183089 0 None -44 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 833 17 2 7 8.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4802913 183089 0 None -44 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 833 17 2 7 8.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
2229 460 17 None -3 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
295 460 17 None -3 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
CHEMBL128365 460 17 None -3 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
164620907 187963 0 None -10232 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4865939 187963 0 None -10232 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028619 187963 0 None -10232 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
162353374 179463 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.2 CC1CCCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4747590 179463 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.2 CC1CCCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
162353394 180188 0 None -1 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 245 2 0 3 1.5 O=C(CN1CCCc2cnccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4756237 180188 0 None -1 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 245 2 0 3 1.5 O=C(CN1CCCc2cnccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
156015895 177706 0 None -6 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 993 21 2 8 10.7 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4643290 177706 0 None -6 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 993 21 2 8 10.7 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650874 177706 0 None -6 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 993 21 2 8 10.7 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
137636830 160677 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 4 0 1 2.5 COc1cccc(C2CC2C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4061384 160677 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 4 0 1 2.5 COc1cccc(C2CC2C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4117956 160677 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 4 0 1 2.5 COc1cccc(C2CC2C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
44448498 12233 0 None -3 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 534 12 2 4 6.0 OC(CCCN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185287 12233 0 None -3 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 534 12 2 4 6.0 OC(CCCN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL404866 12233 0 None -3 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 534 12 2 4 6.0 OC(CCCN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
2284 3133 27 None -10 28 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3133 27 None -10 28 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3133 27 None -10 28 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3133 27 None -10 28 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3133 27 None -10 28 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
44437308 12221 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 285 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc2C1 10.1016/j.bmc.2007.09.003
CHEMBL1185188 12221 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 285 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc2C1 10.1016/j.bmc.2007.09.003
CHEMBL396845 12221 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 285 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc2C1 10.1016/j.bmc.2007.09.003
44309090 202054 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 6 3 3 2.8 O=C(NCCC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL67873 202054 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 6 3 3 2.8 O=C(NCCC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
57339144 91806 71 None -12 5 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM3Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM3
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 nan
CHEMBL2426364 91806 71 None -12 5 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM3Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM3
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 nan
11809446 59367 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL172234 59367 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
57326237 76830 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042407 76830 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078985 76830 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
44337748 9305 0 None 1 2 Rat 5.1 pKi = 5.1 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL111529 9305 0 None 1 2 Rat 5.1 pKi = 5.1 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
16125591 84274 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 455 6 2 2 3.8 C[N+]1(CC(=O)Nc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222634 84274 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 455 6 2 2 3.8 C[N+]1(CC(=O)Nc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
90666118 108864 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 702 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CC[C@@H](OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219051 108864 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 702 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CC[C@@H](OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
44337761 9100 0 None -3 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL110339 9100 0 None -3 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
44443731 93778 0 None 36 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 7 2 3 3.4 O=C(N[C@H]1[C@@H]2CN(CCc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL249830 93778 0 None 36 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 7 2 3 3.4 O=C(N[C@H]1[C@@H]2CN(CCc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
44627860 13921 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197371 13921 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL568870 13921 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
53326934 58212 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 422 11 1 3 7.1 CCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683917 58212 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 422 11 1 3 7.1 CCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
44308900 202298 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 367 5 2 4 1.4 NCCN1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL69582 202298 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 367 5 2 4 1.4 NCCN1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
277 1274 55 None -11 45 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1274 55 None -11 45 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1274 55 None -11 45 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1274 55 None -11 45 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1274 55 None -11 45 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
59291578 112288 0 None -1 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 313 3 1 5 3.0 O=C(Nc1ncoc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298594 112288 0 None -1 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 313 3 1 5 3.0 O=C(Nc1ncoc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305763 112288 0 None -1 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 313 3 1 5 3.0 O=C(Nc1ncoc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
214124 169124 2 None -2 4 Human 8.0 pKi = 8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Muscarinic acetylcholine receptor M3 subtype
ChEMBL 331 8 0 3 4.4 CCN(CC)CCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL443780 169124 2 None -2 4 Human 8.0 pKi = 8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Muscarinic acetylcholine receptor M3 subtype
ChEMBL 331 8 0 3 4.4 CCN(CC)CCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
135409468 2004 63 None -32 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 2004 63 None -32 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 2004 63 None -32 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
155515662 169397 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 336 4 0 3 3.9 O=C(OCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4441786 169397 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 336 4 0 3 3.9 O=C(OCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
10862395 4957 0 None -22 5 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 406 4 1 5 4.4 CCOC(=O)c1c(CC)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL105148 4957 0 None -22 5 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 406 4 1 5 4.4 CCOC(=O)c1c(CC)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
11004046 5381 0 None -60 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 406 3 0 6 4.1 CCOC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL107444 5381 0 None -60 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 406 3 0 6 4.1 CCOC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
2551 782 23 None -54 11 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
11057 175575 19 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 175575 19 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 175575 19 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 175575 19 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
71716224 86528 0 None 1 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 317 4 0 5 1.9 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)Cc3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323444 86528 0 None 1 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 317 4 0 5 1.9 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)Cc3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
130442480 174698 0 None -112 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174698 0 None -112 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
16125443 84226 0 None 3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 335 3 1 2 3.1 CN1CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061159a
CHEMBL222402 84226 0 None 3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 335 3 1 2 3.1 CN1CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061159a
44308818 101611 0 None 2 3 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 360 5 3 3 3.4 NCc1cccc(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)c1 10.1016/s0960-894x(03)00350-0
CHEMBL302145 101611 0 None 2 3 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 360 5 3 3 3.4 NCc1cccc(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)c1 10.1016/s0960-894x(03)00350-0
10598540 38094 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 426 6 2 3 5.0 O=C(NC1CCN(CC2CCCCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL146291 38094 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 426 6 2 3 5.0 O=C(NC1CCN(CC2CCCCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
324 1894 12 None -17 9 Human 7.0 pKi = 7.0 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(01)00186-x
6436265 1894 12 None -17 9 Human 7.0 pKi = 7.0 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(01)00186-x
CHEMBL277642 1894 12 None -17 9 Human 7.0 pKi = 7.0 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(01)00186-x
324 1894 12 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
6436265 1894 12 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
CHEMBL277642 1894 12 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
118719920 115273 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 509 10 0 7 4.5 CN1CCC=C(c2nsnc2OCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354066 115273 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 509 10 0 7 4.5 CN1CCC=C(c2nsnc2OCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
44308799 202331 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 6 1 3 3.5 CN(C)CCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL69765 202331 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 6 1 3 3.5 CN(C)CCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
164614994 187918 0 None -776 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 930 23 9 12 0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4850553 187918 0 None -776 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 930 23 9 12 0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028287 187918 0 None -776 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 930 23 9 12 0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
124087 1362 106 None -9 15 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1362 106 None -9 15 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1362 106 None -9 15 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1362 106 None -9 15 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1362 106 None -9 15 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
10660 14298 55 None -2 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 14298 55 None -2 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
11759212 57586 0 None -117 6 Human 7.0 pKi = 7.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
CHEMBL167223 57586 0 None -117 6 Human 7.0 pKi = 7.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
44627739 196695 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 333 4 1 3 4.3 CN1CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL576663 196695 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 333 4 1 3 4.3 CN1CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
611066 156967 1 None -3 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 381 4 2 6 0.9 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCO)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL407975 156967 1 None -3 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 381 4 2 6 0.9 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCO)CC2)c2ccccc21 10.1021/jm00111a032
71716225 86529 0 None -1 2 Rat 4.0 pKi = 4.0 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 317 4 0 5 1.9 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)Cc3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323445 86529 0 None -1 2 Rat 4.0 pKi = 4.0 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 317 4 0 5 1.9 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)Cc3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
11834199 58463 0 None -21 5 Human 6.0 pKi = 6.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCN(CC)CCC1=C(C(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL168704 58463 0 None -21 5 Human 6.0 pKi = 6.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCN(CC)CCC1=C(C(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
155513986 175913 0 None -562 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 19 10 8 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4439675 175913 0 None -562 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 19 10 8 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596667 175913 0 None -562 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 19 10 8 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
154734599 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
327 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
4108 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
CHEMBL27673 2467 8 None -66 11 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
164620270 187957 0 None -8128 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4869723 187957 0 None -8128 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028587 187957 0 None -8128 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
162670602 182355 0 None -1 2 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 248 2 0 2 1.8 O=C(CN1CCc2ccc(F)cc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4792675 182355 0 None -1 2 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 248 2 0 2 1.8 O=C(CN1CCc2ccc(F)cc21)N1CCCC1 10.1016/j.bmcl.2020.127632
202119 11930 3 None -1 3 Rat 5.0 pKi = 5.0 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL1183388 11930 3 None -1 3 Rat 5.0 pKi = 5.0 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL294470 11930 3 None -1 3 Rat 5.0 pKi = 5.0 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
44443721 93827 0 None 14 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 390 6 2 3 3.3 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL250203 93827 0 None 14 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 390 6 2 3 3.3 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
5353853 17803 41 None -13 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17803 41 None -13 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17803 41 None -13 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
44400218 67287 0 None 2 2 Rat 6.0 pKi = 6.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 383 6 1 5 2.6 COc1ccc(C(O)(C(=O)OCC#CCN2CC3CC3C2)C2CCCC2)cc1 10.1016/j.bmcl.2005.02.036
CHEMBL190459 67287 0 None 2 2 Rat 6.0 pKi = 6.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 383 6 1 5 2.6 COc1ccc(C(O)(C(=O)OCC#CCN2CC3CC3C2)C2CCCC2)cc1 10.1016/j.bmcl.2005.02.036
10865439 20425 0 None -10 5 Human 7.0 pKi = 7.0 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 715 15 0 6 7.6 COc1ccccc1CN1CCC(C2CCN(C(=O)CCCCCCC(=O)N3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
CHEMBL130835 20425 0 None -10 5 Human 7.0 pKi = 7.0 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 715 15 0 6 7.6 COc1ccccc1CN1CCC(C2CCN(C(=O)CCCCCCC(=O)N3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
135466875 188526 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 769 25 5 10 6.6 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
CHEMBL510340 188526 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 769 25 5 10 6.6 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
15050950 202359 0 None -1 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 422 5 2 6 1.1 CC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL70003 202359 0 None -1 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 422 5 2 6 1.1 CC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
109014373 179222 1 None -10 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCN(C(=O)CCN2CCCc3ccccc32)CC1 10.1016/j.bmcl.2020.127632
CHEMBL4744856 179222 1 None -10 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCN(C(=O)CCN2CCCc3ccccc32)CC1 10.1016/j.bmcl.2020.127632
156011112 177700 0 None -4 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4633679 177700 0 None -4 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650842 177700 0 None -4 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
10418420 69930 0 None -74 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 955 27 0 10 10.9 CN(CCCCCCCCN(C)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00113-8
CHEMBL194216 69930 0 None -74 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 955 27 0 10 10.9 CN(CCCCCCCCN(C)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00113-8
57326144 76838 0 None -1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042402 76838 0 None -1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079061 76838 0 None -1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm2013216
44274477 165016 0 None -3 5 Human 4.0 pKi = 4.0 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 331 2 0 3 2.8 CN1CCN(C(=O)C2=C/C(=C\c3ccncc3)c3ccccc32)CC1 10.1016/s0960-894x(01)00186-x
CHEMBL424214 165016 0 None -3 5 Human 4.0 pKi = 4.0 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 331 2 0 3 2.8 CN1CCN(C(=O)C2=C/C(=C\c3ccncc3)c3ccccc32)CC1 10.1016/s0960-894x(01)00186-x
53326849 58219 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 381 8 2 4 4.5 NCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683923 58219 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 381 8 2 4 4.5 NCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
657255 197406 29 None -11 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 197406 29 None -11 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
10984804 98024 0 None 30 2 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NC[C@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL275914 98024 0 None 30 2 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NC[C@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
2551 782 23 None -54 11 Rat 6.0 pKi = 6 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 782 23 None -54 11 Rat 6.0 pKi = 6 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 782 23 None -54 11 Rat 6.0 pKi = 6 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 782 23 None -54 11 Rat 6.0 pKi = 6 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 782 23 None -54 11 Rat 6.0 pKi = 6 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
154734599 2467 8 None -66 11 Rat 6.0 pKi = 6 Binding
Compound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary glandCompound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm970740r
327 2467 8 None -66 11 Rat 6.0 pKi = 6 Binding
Compound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary glandCompound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm970740r
4108 2467 8 None -66 11 Rat 6.0 pKi = 6 Binding
Compound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary glandCompound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm970740r
CHEMBL27673 2467 8 None -66 11 Rat 6.0 pKi = 6 Binding
Compound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary glandCompound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm970740r
154059 3580 49 None -1 8 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
2457 3580 49 None -1 8 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
7483 3580 49 None -1 8 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
CHEMBL1734 3580 49 None -1 8 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
DB01591 3580 49 None -1 8 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
306 3400 18 None -4 5 Human 8.1 pIC50 = 8.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
3536 3400 18 None -4 5 Human 8.1 pIC50 = 8.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
53930639 3400 18 None -4 5 Human 8.1 pIC50 = 8.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
9577995 3400 18 None -4 5 Human 8.1 pIC50 = 8.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
CHEMBL134641 3400 18 None -4 5 Human 8.1 pIC50 = 8.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
2745 3800 39 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3800 39 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3800 39 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3800 39 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3800 39 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3800 39 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
2824 3930 0 None 1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
345 3930 0 None 1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
71203 3930 0 None 1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
CHEMBL1892145 3930 0 None 1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
DB13793 3930 0 None 1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
92112 21505 14 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@@]12CCCN3CCc4c(n(c5ccccc45)C(=O)C1)[C@H]32 None
CHEMBL1318553 21505 14 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@@]12CCCN3CCc4c(n(c5ccccc45)C(=O)C1)[C@H]32 None
2360 3637 41 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
2484 3637 41 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
347 3637 41 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
441071 3637 41 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
CHEMBL227934 3637 41 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
DB15954 3637 41 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
15376 3931 0 None 1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
349 3931 0 None 1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
3643 3931 0 None 1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
CHEMBL1165342 3931 0 None 1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
DB13374 3931 0 None 1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
21158560 112296 4 None -1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 666 6 2 4 5.5 C=CC[N@@+]12CC[C@@]34c5ccccc5N5/C=C6/[C@H]7C[C@H]8[C@@]9(CC[N@@+]8(CC=C)C/C7=C/CO)c7ccccc7N(/C=C(/[C@@H](C[C@@H]31)/C(=C\CO)C2)[C@H]54)[C@@H]69 None
CHEMBL3305985 112296 4 None -1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 666 6 2 4 5.5 C=CC[N@@+]12CC[C@@]34c5ccccc5N5/C=C6/[C@H]7C[C@H]8[C@@]9(CC[N@@+]8(CC=C)C/C7=C/CO)c7ccccc7N(/C=C(/[C@@H](C[C@@H]31)/C(=C\CO)C2)[C@H]54)[C@@H]69 None
2381 656 43 None -9 9 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
374 656 43 None -9 9 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
7128 656 43 None -9 9 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
CHEMBL1101 656 43 None -9 9 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
DB00810 656 43 None -9 9 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
656598 216020 0 None -1 4 Rat 8.1 pKd = 8.1 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
Drug Central 304 4 1 3 2.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C2)OC(=O)[C@@H](CO)C1=CC=CC=C1 None
11968014 12649 4 None -1 9 Rat 8.0 pKd = 8.0 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
Drug Central 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 None
CHEMBL1187846 12649 4 None -1 9 Rat 8.0 pKd = 8.0 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
Drug Central 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 None
319 1297 39 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
321 1297 39 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
444031 1297 39 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
784 1297 39 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
CHEMBL1346 1297 39 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
DB00496 1297 39 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
12165 898 4 None -15 2 Human 10.2 pKd = 10.2 Binding
Binding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracerBinding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracer
Guide to Pharmacology 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 35901125
90200922 898 4 None -15 2 Human 10.2 pKd = 10.2 Binding
Binding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracerBinding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracer
Guide to Pharmacology 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 35901125
CHEMBL5172865 898 4 None -15 2 Human 10.2 pKd = 10.2 Binding
Binding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracerBinding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracer
Guide to Pharmacology 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 35901125
23056 112 26 None -1 7 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 3443095
23056 112 26 None -1 7 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
318 112 26 None -1 7 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 3443095
318 112 26 None -1 7 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
3260 112 26 None -1 7 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 3443095
3260 112 26 None -1 7 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
CHEMBL12980 112 26 None -1 7 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 3443095
CHEMBL12980 112 26 None -1 7 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
367 3764 8 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
5487427 3764 8 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
8592 3764 8 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
CHEMBL1900528 3764 8 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
CHEMBL3305968 3764 8 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
CHEMBL4650755 3764 8 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
DB01409 3764 8 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
344 2708 0 None -19 5 Human 3.3 pKd = 3.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 3 0 4 2.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)CCl 9495826
44358908 2708 0 None -19 5 Human 3.3 pKd = 3.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 3 0 4 2.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)CCl 9495826
CHEMBL139677 2708 0 None -19 5 Human 3.3 pKd = 3.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 3 0 4 2.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)CCl 9495826
15118529 4020 0 None -6 4 Human 5.1 pKd = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 0 1 4 5.4 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CCC2=Cc3c(C[C@]12C)cn1c(n3)nc2c1cccc2 12435818
340 4020 0 None -6 4 Human 5.1 pKd = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 0 1 4 5.4 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CCC2=Cc3c(C[C@]12C)cn1c(n3)nc2c1cccc2 12435818
CHEMBL1256845 4020 0 None -6 4 Human 5.1 pKd = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 0 1 4 5.4 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CCC2=Cc3c(C[C@]12C)cn1c(n3)nc2c1cccc2 12435818
2381 656 43 None -9 9 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
374 656 43 None -9 9 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
7128 656 43 None -9 9 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
CHEMBL1101 656 43 None -9 9 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
DB00810 656 43 None -9 9 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
319 1297 39 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
321 1297 39 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
444031 1297 39 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
784 1297 39 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
CHEMBL1346 1297 39 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
DB00496 1297 39 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
316 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
316 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
316 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
316 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
316 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
316 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
317 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
317 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
317 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
317 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
317 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
317 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
71183 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
71183 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
71183 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
71183 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
71183 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
71183 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
CHEMBL3140030 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
CHEMBL3140030 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
CHEMBL3140030 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
CHEMBL3140030 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
CHEMBL3140030 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
CHEMBL3140030 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
CHEMBL376897 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
CHEMBL376897 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
CHEMBL376897 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
CHEMBL376897 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
CHEMBL376897 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
CHEMBL376897 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
DB00462 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
DB00462 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
DB00462 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
DB00462 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
DB00462 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
DB00462 2793 14 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
316 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
316 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
317 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
317 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
71183 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
71183 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
CHEMBL3140030 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
CHEMBL3140030 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
CHEMBL376897 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
CHEMBL376897 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
DB00462 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
DB00462 2793 14 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
21123938 724 0 None -12 5 Human 2.5 pKd None 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N@@+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)[O-] 9495826
343 724 0 None -12 5 Human 2.5 pKd None 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N@@+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)[O-] 9495826
342 723 50 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9224827
342 723 50 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9495826
442021 723 50 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9224827
442021 723 50 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9495826
CHEMBL501756 723 50 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9224827
CHEMBL501756 723 50 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9495826
332 2003 0 None -10 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 4 3.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)Cc1ccccc1 9495826
44358893 2003 0 None -10 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 4 3.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)Cc1ccccc1 9495826
CHEMBL343796 2003 0 None -10 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 4 3.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)Cc1ccccc1 9495826
348 3743 0 None 1 4 Human 4.4 pKd None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 2 1 6 1.9 OCCc1sc2=Nc3c(Cn2c1C)cnc(n3)C 14722259
66706 3743 0 None 1 4 Human 4.4 pKd None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 2 1 6 1.9 OCCc1sc2=Nc3c(Cn2c1C)cnc(n3)C 14722259
2360 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
2360 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
2484 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
2484 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
347 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
347 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
441071 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
441071 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
CHEMBL227934 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
CHEMBL227934 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
DB15954 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
DB15954 3637 41 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
335 1806 0 None -5 4 Human 5.1 pKd None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 470 5 2 7 3.3 COc1ccc2c(c1)c1c3c(=O)[nH]c(=O)c3c3c(c1n2CC(CN(C)C)O)n(C)c1c3cccc1 10860942
3500 1806 0 None -5 4 Human 5.1 pKd None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 470 5 2 7 3.3 COc1ccc2c(c1)c1c3c(=O)[nH]c(=O)c3c3c(c1n2CC(CN(C)C)O)n(C)c1c3cccc1 10860942
CHEMBL157822 1806 0 None -5 4 Human 5.1 pKd None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 470 5 2 7 3.3 COc1ccc2c(c1)c1c3c(=O)[nH]c(=O)c3c3c(c1n2CC(CN(C)C)O)n(C)c1c3cccc1 10860942
2824 3930 0 None 1 4 Human 5.2 pKd None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
345 3930 0 None 1 4 Human 5.2 pKd None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
71203 3930 0 None 1 4 Human 5.2 pKd None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
CHEMBL1892145 3930 0 None 1 4 Human 5.2 pKd None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
DB13793 3930 0 None 1 4 Human 5.2 pKd None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
339 4018 0 None -5 4 Human 5.5 pKd None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 0 1 4 5.2 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC[C@@H]2[C@]1(C)Cc1cn3c(nc1C2)nc1c3cccc1 12435818
9803245 4018 0 None -5 4 Human 5.5 pKd None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 0 1 4 5.2 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC[C@@H]2[C@]1(C)Cc1cn3c(nc1C2)nc1c3cccc1 12435818
CHEMBL2206331 4018 0 None -5 4 Human 5.5 pKd None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 0 1 4 5.2 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC[C@@H]2[C@]1(C)Cc1cn3c(nc1C2)nc1c3cccc1 12435818
15376 3931 0 None 1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
349 3931 0 None 1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
3643 3931 0 None 1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
CHEMBL1165342 3931 0 None 1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
DB13374 3931 0 None 1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
341 337 0 None -5 4 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 666 6 2 4 5.5 C=CC[N+]12CC[C@@]34[C@@H]2C[C@@H](C(=CCO)C1)C1=CN2c5ccccc5[C@]56[C@@H]2C(=CN([C@H]31)c1c4cccc1)[C@H]1C[C@@H]6[N+](CC1=CCO)(CC5)CC=C 9224827
5311001 337 0 None -5 4 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 666 6 2 4 5.5 C=CC[N+]12CC[C@@]34[C@@H]2C[C@@H](C(=CCO)C1)C1=CN2c5ccccc5[C@]56[C@@H]2C(=CN([C@H]31)c1c4cccc1)[C@H]1C[C@@H]6[N+](CC1=CCO)(CC5)CC=C 9224827
23056 112 26 3H-QNB -1 7 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
318 112 26 3H-QNB -1 7 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
3260 112 26 3H-QNB -1 7 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
CHEMBL12980 112 26 3H-QNB -1 7 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
23056 112 26 3H-QNB -1 7 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
318 112 26 3H-QNB -1 7 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
3260 112 26 3H-QNB -1 7 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
CHEMBL12980 112 26 3H-QNB -1 7 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
12057539 206301 39 3H-Arachidonic Acid 1 20 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-Arachidonic Acid 1 20 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-Arachidonic Acid 1 20 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
12057539 206301 39 3H-NMS 1 20 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-NMS 1 20 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-NMS 1 20 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
131632304 214266 0 3H-NMS -1 13 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
12057539 206301 39 3H-QNB 1 20 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-QNB 1 20 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-QNB 1 20 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
44431393 87596 0 UNDEFINED -1 3 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 402 6 1 5 3.5 CN(C)C1(CNCCC2CCOCC2)COc2cc(Cl)c(Cl)cc2OC1 None
CHEMBL234440 87596 0 UNDEFINED -1 3 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 402 6 1 5 3.5 CN(C)C1(CNCCC2CCOCC2)COc2cc(Cl)c(Cl)cc2OC1 None
12057539 206301 39 3H-NMS -2 20 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-NMS -2 20 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-NMS -2 20 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
325 2031 0 3H-NMS -1 9 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
3746 2031 0 3H-NMS -1 9 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
657308 2031 0 3H-NMS -1 9 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
CHEMBL1615433 2031 0 3H-NMS -1 9 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
DB00332 2031 0 3H-NMS -1 9 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
12057539 206301 39 3H-PIRENZEPINE -2 20 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-PIRENZEPINE -2 20 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-PIRENZEPINE -2 20 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
131632304 214266 0 3H-QNB -3 13 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
1734 116 8 3H-4-DAMP 1 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 8 3H-4-DAMP 1 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 8 3H-4-DAMP 1 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
12057539 206301 39 3H-NMS 1 20 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-NMS 1 20 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-NMS 1 20 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
325 2031 0 3H-NMS -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
3746 2031 0 3H-NMS -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
657308 2031 0 3H-NMS -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
CHEMBL1615433 2031 0 3H-NMS -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
DB00332 2031 0 3H-NMS -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
1734 116 8 3H-NMS 1 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 8 3H-NMS 1 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 8 3H-NMS 1 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
1734 116 8 3H-NMS -2 12 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 8 3H-NMS -2 12 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 8 3H-NMS -2 12 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
2028 2931 77 3H-NMS -1 11 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2931 77 3H-NMS -1 11 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2931 77 3H-NMS -1 11 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2931 77 3H-NMS -1 11 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2931 77 3H-NMS -1 11 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
1734 116 8 3H-QNB 1 12 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 8 3H-QNB 1 12 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 8 3H-QNB 1 12 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
3246155 214183 0 3H-NMS -3 16 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
2028 2931 77 UNDEFINED 1 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2931 77 UNDEFINED 1 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2931 77 UNDEFINED 1 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2931 77 UNDEFINED 1 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2931 77 UNDEFINED 1 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
12057539 206301 39 3H-NMS 1 20 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
12057539 206301 39 3H-NMSP 1 20 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-NMS 1 20 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-NMSP 1 20 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-NMS 1 20 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-NMSP 1 20 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
None 214475 0 3H-NMS 1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 426 7 1 3 4.0 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5 None
1734 116 8 3H-PIRENZEPINE -2 12 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 8 3H-PIRENZEPINE -2 12 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 8 3H-PIRENZEPINE -2 12 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
12057539 206301 39 3H-NMS -2 20 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-NMS -2 20 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-NMS -2 20 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
12057539 206301 39 3H-QNB 1 20 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-QNB 1 20 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-QNB 1 20 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3246155 214183 0 3H-QNB -4 16 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
130169 3548 0 3H-NMS 1 5 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O None
331 3548 0 3H-NMS 1 5 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O None
None 214475 0 3H-NMS -1 6 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 426 7 1 3 4.0 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5 None
44431384 148328 0 UNDEFINED -2 3 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 384 6 1 4 4.0 CN(C)C1(CNCCC23CC4CC(CC(C4)C2)C3)COc2ccccc2OC1 None
CHEMBL394137 148328 0 UNDEFINED -2 3 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 384 6 1 4 4.0 CN(C)C1(CNCCC23CC4CC(CC(C4)C2)C3)COc2ccccc2OC1 None
3042 1386 31 3H-NMS 1 15 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1386 31 3H-NMS 1 15 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1386 31 3H-NMS 1 15 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1386 31 3H-NMS 1 15 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1386 31 3H-NMS 1 15 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
2381 656 43 3H-NMS -3 9 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
374 656 43 3H-NMS -3 9 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
7128 656 43 3H-NMS -3 9 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
CHEMBL1101 656 43 3H-NMS -3 9 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
DB00810 656 43 3H-NMS -3 9 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
2293 3137 23 None -1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
329 3137 23 None -1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
4934 3137 23 None -1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
CHEMBL1180725 3137 23 None -1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
DB00782 3137 23 None -1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
310 1891 0 3H-NMS -3 11 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
3602 1891 0 3H-NMS -3 11 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
CHEMBL3545990 1891 0 3H-NMS -3 11 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
11434515 259 3 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
11519741 259 3 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
4484 259 3 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
7449 259 3 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
CHEMBL1194325 259 3 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
DB08897 259 3 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
11519069 3876 2 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
11519070 3876 2 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
4816 3876 2 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
7354 3876 2 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
CHEMBL1187833 3876 2 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
DB09076 3876 2 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
316 2793 14 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
317 2793 14 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
71183 2793 14 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL3140030 2793 14 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL376897 2793 14 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
DB00462 2793 14 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
154825138 214267 0 3H-4-DAMP -17 12 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
1209 1628 69 3H-QNB -30 31 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1628 69 3H-QNB -30 31 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1628 69 3H-QNB -30 31 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1628 69 3H-QNB -30 31 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1628 69 3H-QNB -30 31 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
214 3799 52 3H-QNB -1202 29 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-QNB -1202 29 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-QNB -1202 29 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-QNB -1202 29 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-QNB -1202 29 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-QNB -1202 29 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
46222048 8896 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
CHEMBL1098230 8896 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
11957621 214268 0 3H-NMS -12 10 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 203 3 2 3 1.3 COC1=C(C=CC(=C1)CCN)O.Cl None
11957621 214268 0 3H-NMS -12 10 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 203 3 2 3 1.3 COC1=C(C=CC(=C1)CCN)O.Cl None
3075702 215594 0 3H-4-DAMP -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
145 140 48 3H-QNB -1949 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 48 3H-QNB -1949 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 48 3H-QNB -1949 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 48 3H-QNB -1949 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
179 396 107 3H-QNB -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-QNB -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-QNB -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-QNB -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-QNB -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
141 1399 32 3H-QNB -114 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1399 32 3H-QNB -114 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1399 32 3H-QNB -114 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1399 32 3H-QNB -114 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
119376 1811 41 3H-DAMP -54954 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 1811 41 3H-DAMP -54954 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 1811 41 3H-DAMP -54954 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
1353 1880 85 3H-QNB -154 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-QNB -154 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-QNB -154 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-QNB -154 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-QNB -154 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3294 1975 106 3H-NMS -14454 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-NMS -14454 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-NMS -14454 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-NMS -14454 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-NMS -14454 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1588 2294 24 3H-QNB -41686 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 3H-QNB -41686 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 3H-QNB -41686 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 3H-QNB -41686 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 3H-QNB -41686 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1830 2552 39 3H-QNB -39 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 2552 39 3H-QNB -1778 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 3H-QNB -39 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 3H-QNB -1778 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 3H-QNB -39 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 3H-QNB -1778 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 3H-QNB -39 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 3H-QNB -1778 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 3H-QNB -39 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 3H-QNB -1778 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
15897 2817 0 3H-QNB -32 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2817 0 3H-QNB -32 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2817 0 3H-QNB -32 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
119570 3110 90 3H-QNB -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3110 90 3H-QNB -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3110 90 3H-QNB -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3110 90 3H-QNB -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3110 90 3H-QNB -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2337 3205 72 3H-QNB -81 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-QNB -81 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-QNB -81 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-QNB -81 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-QNB -81 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2389 3279 114 3H-QNB -575 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-QNB -575 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-QNB -575 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-QNB -575 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-QNB -575 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
128563 3408 28 3H-QNB -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3408 28 3H-QNB -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3408 28 3H-QNB -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3408 28 3H-QNB -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1267 3744 43 3H-NMS -4168 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3744 43 3H-NMS -4168 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3744 43 3H-NMS -4168 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
213 3792 50 3H-QNB -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3792 50 3H-QNB -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3792 50 3H-QNB -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3792 50 3H-QNB -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3792 50 3H-QNB -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
185 3943 54 3H-QNB -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-QNB -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-QNB -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-QNB -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2865 4079 67 3H-QNB -812 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-QNB -812 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-QNB -812 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-QNB -812 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-QNB -812 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
103 4089 56 3H-QNB -144 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-QNB -144 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-QNB -144 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-QNB -144 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-QNB -144 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
10297 26905 29 3H-QNB -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 26905 29 3H-QNB -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
115237 55296 113 3H-QNB -7762 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 3H-QNB -7762 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1979 76973 66 3H-cAMP 2 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 76973 66 3H-cAMP 2 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
3025067 98923 58 3H-NMS -512 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
65853 98923 58 3H-NMS -512 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
CHEMBL282614 98923 58 3H-NMS -512 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
3663 99505 79 3H-QNB -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99505 79 3H-QNB -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
3452843 119020 13 3H-NMS -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
CHEMBL345686 119020 13 3H-NMS -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
446220 132998 13 3H-QNB -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 132998 13 3H-QNB -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
5280343 187691 119 3H-QNB -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 187691 119 3H-QNB -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 187691 119 3H-QNB -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
162265 200587 19 3H-QNB -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 200587 19 3H-QNB -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 200587 19 3H-QNB -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 201336 85 3H-QNB -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 201336 85 3H-QNB -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
5656 201377 82 3H-QNB -79 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 201377 82 3H-QNB -79 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
1973 201790 12 3H-4-DAMP -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 201790 12 3H-4-DAMP -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 201790 12 3H-4-DAMP -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
202478 202981 15 3H-QNB -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 202981 15 3H-QNB -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
5311189 203133 4 3H-QNB -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 203133 4 3H-QNB -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 203630 21 3H-QNB -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 203630 21 3H-QNB -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 203630 21 3H-QNB -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 203790 64 3H-QNB -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 203790 64 3H-QNB -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 203790 64 3H-QNB -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
16231 205776 53 3H-NMS -7 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
CHEMBL945 205776 53 3H-NMS -7 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
11954224 214174 0 3H-QNB -141253 59 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
5831 214185 0 3H-NMS -51 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
5831 214185 0 3H-NMS -2344 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
11954259 214201 0 3H-QNB -13182 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
15387 214209 0 3H-QNB -1479 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
444 214245 0 3H-QNB -2089 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(C(=O)C1=CC(=CC=C1)Cl)NC(C)(C)C None
37632 214375 0 3H-QNB -1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 0 5 3.3 CN(C)CC1=NN=C2N1C3=C(C=C(C=C3)Cl)C(=NC2)C4=CC=CC=C4 None
40589 214376 0 3H-QNB -407 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 377 7 0 6 2.5 CCC1=NN(C(=O)N1CC)CCCN2CCN(CC2)C3=CC(=CC=C3)Cl None
25137849 214425 0 3H-QNB -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 214425 0 3H-QNB -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
3337 214441 0 3H-QNB -158 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214441 0 3H-QNB -158 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214441 0 3H-QNB -158 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214441 0 3H-QNB -158 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
None 214486 0 3H-QNB -38018 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 214555 0 3H-NMS 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 483 7 3 4 4.4 CC(CCC(=O)NCCS(=O)(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C None
None 214555 0 3H-NMS -1 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 483 7 3 4 4.4 CC(CCC(=O)NCCS(=O)(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C None
None 214556 0 3H-NMS 1 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 433 6 3 3 4.6 CC(CCC(=O)NCC(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C None
None 214556 0 3H-NMS -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 433 6 3 3 4.6 CC(CCC(=O)NCC(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C None
None 214560 0 3H-QNB -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 214561 0 3H-QNB -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 214562 0 3H-QNB -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 214563 0 3H-QNB -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 214564 0 3H-QNB -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 214565 0 3H-QNB -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 214566 0 3H-QNB -1 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 214567 0 3H-QNB -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 214574 0 3H-QNB -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 214575 0 3H-QNB -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 214576 0 3H-QNB -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
4978 214577 0 3H-QNB -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 214578 0 3H-QNB -3 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 214579 0 3H-QNB -281 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 214580 0 3H-QNB -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
None 214703 0 UNDEFINED -660 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214753 0 3H-NMS -1 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 7 4 5 1.8 CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O None
214 3799 52 3H-QNB -93 29 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-QNB -93 29 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-QNB -93 29 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-QNB -93 29 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-QNB -93 29 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-QNB -93 29 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2869 108 3H-QNB -27 65 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-QNB -27 65 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-QNB -27 65 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-QNB -27 65 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 944 89 3H-NMS -10 91 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-NMSP -10 91 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-NMS -10 91 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-NMSP -10 91 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-NMS -10 91 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-NMSP -10 91 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-NMS -10 91 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-NMSP -10 91 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-NMS -10 91 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-NMSP -10 91 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
9905731 167943 0 UNDEFINED -1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 334 6 1 5 2.2 CN(C)C1(CNCCC2CCOCC2)COc2ccccc2OC1 None
CHEMBL435353 167943 0 UNDEFINED -1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 334 6 1 5 2.2 CN(C)C1(CNCCC2CCOCC2)COc2ccccc2OC1 None
367 3764 8 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
5487427 3764 8 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
8592 3764 8 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL1900528 3764 8 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL3305968 3764 8 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL4650755 3764 8 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
DB01409 3764 8 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
154734599 2467 8 3H-NMS -19 11 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2467 8 3H-NMS -19 11 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2467 8 3H-NMS -19 11 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2467 8 3H-NMS -19 11 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
277 1274 55 3H-QNB -11 45 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 3H-QNB -11 45 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 3H-QNB -11 45 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 3H-QNB -11 45 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 3H-QNB -11 45 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
4919 204511 21 3H-QNB -2 9 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 204511 21 3H-QNB -2 9 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
180 397 50 3H-QNB -23 38 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-QNB -23 38 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-QNB -23 38 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-QNB -23 38 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-QNB -23 38 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
4601 205020 29 3H-QNB -1 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 205020 29 3H-QNB -1 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 205020 29 3H-QNB -1 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
1613 2316 44 3H-QNB -15 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-QNB -15 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-QNB -15 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-QNB -15 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-QNB -15 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2200 3082 38 3H-4-DAMP -15 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-4-DAMP -15 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-4-DAMP -15 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-4-DAMP -15 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-4-DAMP -15 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
154825138 214267 0 3H-PIRENZEPINE -30 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
442108 84213 5 3H-QNB -1 11 Human 4.9 pKi = 4.9 Binding
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
CHEMBL222287 84213 5 3H-QNB -1 11 Human 4.9 pKi = 4.9 Binding
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
135398745 2869 108 35S-GTPGammaS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 35S-GTPGammaS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 35S-GTPGammaS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 35S-GTPGammaS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2745 3800 39 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3800 39 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3800 39 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3800 39 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3800 39 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3800 39 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
101 3762 18 3H-QNB -2041 13 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
55752 3762 18 3H-QNB -2041 13 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL35057 3762 18 3H-QNB -2041 13 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
2337 3205 72 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398745 2869 108 3H-NMS -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2869 108 3H-QNB -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-NMS -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-QNB -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-NMS -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-QNB -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-NMS -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-QNB -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3947 214378 0 3H-QNB -4 15 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1C2=CC=CC=C2CCC3=CC=CC=C31)CC(=O)C4=CC=C(C=C4)Cl None
2865 4079 67 3H-QNB -812 53 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-QNB -812 53 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-QNB -812 53 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-QNB -812 53 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-QNB -812 53 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
68617 203816 60 3H-QNB -12 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 203816 60 3H-QNB -12 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 203816 60 3H-QNB -12 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
154734599 2467 8 3H-NMS -66 11 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2467 8 3H-NMS -66 11 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2467 8 3H-NMS -66 11 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2467 8 3H-NMS -66 11 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
135398745 2869 108 3H-NMS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2869 108 3H-NMSP -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-NMS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-NMSP -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-NMS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-NMSP -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-NMS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-NMSP -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2337 3205 72 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3205 72 3H-NMS -257 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-NMS -257 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-NMS -257 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-NMS -257 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-NMS -257 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2200 3082 38 3H-NMS -15 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-NMS -15 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-NMS -15 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-NMS -15 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-NMS -15 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
135398737 944 89 3H-NMS -7 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-QNB -7 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-NMS -7 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-QNB -7 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-NMS -7 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-QNB -7 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-NMS -7 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-QNB -7 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-NMS -7 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-QNB -7 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
44431386 148493 0 UNDEFINED -1 3 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 332 5 1 5 2.1 CN(C)C1(CNCC=C2CCOCC2)COc2ccccc2OC1 None
CHEMBL394255 148493 0 UNDEFINED -1 3 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 332 5 1 5 2.1 CN(C)C1(CNCC=C2CCOCC2)COc2ccccc2OC1 None
154825138 214267 0 3H-NMS -17 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
154734599 2467 8 3H-NMS -66 11 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2467 8 3H-NMS -66 11 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2467 8 3H-NMS -66 11 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2467 8 3H-NMS -66 11 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
10090005 214210 0 3H-QNB -501 10 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 361 1 0 3 4.4 CN1CCN(CC1)C2=CC3=C(C=CC(=C3)Cl)C(=CC#N)C4=CC=CC=C42 None
154825138 214267 0 3H-NMS -30 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
1212 1632 45 3H-QNB -407 65 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-QNB -407 65 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-QNB -407 65 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-QNB -407 65 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-QNB -407 65 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 1632 45 3H-QNB -2884 65 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-QNB -2884 65 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-QNB -2884 65 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-QNB -2884 65 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-QNB -2884 65 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
100 3745 52 3H-QNB -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-QNB -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-QNB -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-QNB -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-QNB -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
None 214505 0 3H-NMS 1 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 851 24 12 12 -2.6 CCC(C)C(C(=O)NC(CC(=O)O)C(=O)O)NC(=O)C(CO)NC(=O)C(CC1=CN=CN1)NC(=O)C(CC2=CN=CN2)NC(=O)C(CC3=CC=CC=C3)NC(=O)C4CCCN4 None
None 214505 0 3H-4-DAMP 1 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 851 24 12 12 -2.6 CCC(C)C(C(=O)NC(CC(=O)O)C(=O)O)NC(=O)C(CO)NC(=O)C(CC1=CN=CN1)NC(=O)C(CC2=CN=CN2)NC(=O)C(CC3=CC=CC=C3)NC(=O)C4CCCN4 None
2200 3082 38 3H-QNB -15 13 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-QNB -15 13 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-QNB -15 13 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-QNB -15 13 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-QNB -15 13 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
15387 214209 0 3H-QNB -2238 23 Rat 4.8 pKi = 4.8 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
4839 214625 0 3H-NMS -4 5 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 5 0 3 3.8 CCN1CCCC(C1)OC(=O)C(C2=CC=CC=C2)C3=CC=CC=C3 None
15897 2817 0 3H-QNB -32 36 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2817 0 3H-QNB -32 36 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2817 0 3H-QNB -32 36 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
2200 3082 38 3H-PIRENZEPINE -22 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-PIRENZEPINE -22 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-PIRENZEPINE -22 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-PIRENZEPINE -22 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-PIRENZEPINE -22 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
None 214486 0 3H-QNB -38018 29 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
124226 1890 0 3H-NMS -1 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
322 1890 0 3H-NMS -1 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
71202 214621 0 3H-NMS -5 5 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 340 3 0 3 4.9 CC1(C2=CC=CC=C2N(C3=CC=CC=C31)C(=O)SCCN(C)C)C None
1353 1880 85 3H-NMS -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-QNB -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-NMS -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-QNB -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-NMS -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-QNB -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-NMS -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-QNB -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-NMS -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-QNB -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
11954259 214201 0 3H-QNB -13182 43 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
154734599 2467 8 3H-NMS -66 11 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2467 8 3H-NMS -66 11 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2467 8 3H-NMS -66 11 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2467 8 3H-NMS -66 11 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
2200 3082 38 3H-NMS -22 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-NMS -22 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-NMS -22 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-NMS -22 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-NMS -22 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
44431369 87555 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 6 1 4 2.9 Cc1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 None
CHEMBL234253 87555 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 6 1 4 2.9 Cc1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 None
2200 3082 38 3H-NMS -15 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-NMS -15 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-NMS -15 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-NMS -15 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-NMS -15 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
132947 3803 8 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
361 3803 8 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
CHEMBL265256 3803 8 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
209 3008 94 3H-QNB -144 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 3H-QNB -144 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 3H-QNB -144 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 3H-QNB -144 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 3H-QNB -144 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1615 167228 22 3H-QNB -5 44 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167228 22 3H-QNB -5 44 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
209 3008 94 3H-QNB -2630 23 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 3H-QNB -2630 23 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 3H-QNB -2630 23 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 3H-QNB -2630 23 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 3H-QNB -2630 23 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
44431376 86889 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 344 6 1 4 2.7 CN(C)C1(CNCCc2ccccc2F)COc2ccccc2OC1 None
CHEMBL233200 86889 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 344 6 1 4 2.7 CN(C)C1(CNCCc2ccccc2F)COc2ccccc2OC1 None
2337 3205 72 3H-QNB -81 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-QNB -81 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-QNB -81 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-QNB -81 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-QNB -81 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
16362 3076 67 3H-QNB -10232 29 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-QNB -10232 29 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-QNB -10232 29 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-QNB -10232 29 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-QNB -10232 29 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
16362 3076 67 3H-QNB -562 29 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-QNB -562 29 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-QNB -562 29 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-QNB -562 29 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-QNB -562 29 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
154734599 2467 8 3H-4-DAMP -19 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2467 8 3H-4-DAMP -19 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2467 8 3H-4-DAMP -19 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2467 8 3H-4-DAMP -19 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
12057539 206301 39 3H-NMS -2 20 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-NMS -2 20 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-NMS -2 20 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
None 214475 0 3H-NMS -1 6 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 426 7 1 3 4.0 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5 None
16721019 87558 0 UNDEFINED -1 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 7 2 5 2.5 CN(C)C1(CNCCC2CCC(CO)CC2)COc2ccccc2OC1 None
CHEMBL234258 87558 0 UNDEFINED -1 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 7 2 5 2.5 CN(C)C1(CNCCC2CCC(CO)CC2)COc2ccccc2OC1 None
12057539 206301 39 3H-NMS -2 20 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-NMS -2 20 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-NMS -2 20 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
None 214504 0 3H-NMS -1 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 3 1 2 3.9 C1CCC(CC1)C(C#CCN2CCCCC2)(C3=CC=CC=C3)O None
1734 116 8 3H-NMS -2 12 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 8 3H-NMS -2 12 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 8 3H-NMS -2 12 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
2745 3800 39 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3800 39 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3800 39 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3800 39 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3800 39 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3800 39 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
44431382 87593 0 UNDEFINED 2 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 332 6 1 4 3.3 CN(C)C1(CNCCC2CCCCC2)COc2ccccc2OC1 None
CHEMBL234438 87593 0 UNDEFINED 2 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 332 6 1 4 3.3 CN(C)C1(CNCCC2CCCCC2)COc2ccccc2OC1 None
2905 214622 0 3H-NMS -1 5 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 291 6 1 4 2.2 CN(C)CCOC(=O)C(C1=CC=CC=C1)C2(CCCC2)O None
44431383 87594 0 UNDEFINED -1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 346 6 1 4 3.7 CN(C)C1(CNCCC2CCCCCC2)COc2ccccc2OC1 None
CHEMBL234439 87594 0 UNDEFINED -1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 346 6 1 4 3.7 CN(C)C1(CNCCC2CCCCCC2)COc2ccccc2OC1 None
1734 116 8 3H-NMS -2 12 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 8 3H-NMS -2 12 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 8 3H-NMS -2 12 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
44431389 145618 0 UNDEFINED -1 3 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 348 6 2 5 2.3 CN(C)C1(CNCCC2CCC(O)CC2)COc2ccccc2OC1 None
CHEMBL391977 145618 0 UNDEFINED -1 3 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 348 6 2 5 2.3 CN(C)C1(CNCCC2CCC(O)CC2)COc2ccccc2OC1 None
2745 3800 39 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3800 39 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3800 39 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3800 39 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3800 39 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3800 39 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
135398737 944 89 3H-QNB -10 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-QNB -10 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-QNB -10 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-QNB -10 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-QNB -10 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
44431367 87554 0 UNDEFINED 4 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 6 1 4 2.6 CN(C)C1(CNCCc2ccccc2)COc2ccccc2OC1 None
CHEMBL234252 87554 0 UNDEFINED 4 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 6 1 4 2.6 CN(C)C1(CNCCc2ccccc2)COc2ccccc2OC1 None
44431370 87556 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 360 6 1 4 3.2 CN(C)C1(CNCCc2ccc(Cl)cc2)COc2ccccc2OC1 None
CHEMBL234254 87556 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 360 6 1 4 3.2 CN(C)C1(CNCCc2ccc(Cl)cc2)COc2ccccc2OC1 None
5831 214185 0 3H-QNB -51 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
11976 907 54 3H-QNB -20 23 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 3H-QNB -20 23 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 3H-QNB -20 23 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 3H-QNB -20 23 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
2995 202700 49 3H-QNB -5 22 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 202700 49 3H-QNB -5 22 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 202700 49 3H-QNB -5 22 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
154734599 2467 8 3H-NMS -19 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2467 8 3H-NMS -19 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2467 8 3H-NMS -19 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2467 8 3H-NMS -19 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
11976 907 54 3H-QNB -12 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 3H-QNB -12 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 3H-QNB -12 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 3H-QNB -12 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1979 76973 66 3H-cAMP 2 4 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 76973 66 3H-cAMP 2 4 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
2200 3082 38 3H-NMS -15 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-NMS -15 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-NMS -15 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-NMS -15 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-NMS -15 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
132947 3803 8 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
361 3803 8 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
CHEMBL265256 3803 8 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
3012003 214377 0 3H-QNB -1 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 311 5 0 3 3.8 CN1CCC(C(C1)COC2=CC=C(C=C2)OC)C3=CC=CC=C3 None
2200 3082 38 3H-NMS -22 13 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-NMS -22 13 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-NMS -22 13 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-NMS -22 13 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-NMS -22 13 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
1224 1404 79 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1404 79 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1404 79 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1404 79 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1404 79 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1404 79 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
44431375 86888 0 UNDEFINED 2 3 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 394 6 1 4 3.9 CN(C)C1(CNCCc2c(Cl)cccc2Cl)COc2ccccc2OC1 None
CHEMBL233199 86888 0 UNDEFINED 2 3 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 394 6 1 4 3.9 CN(C)C1(CNCCc2c(Cl)cccc2Cl)COc2ccccc2OC1 None
None 214366 0 3H-QNB -2398 23 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
100 3745 52 3H-QNB -12 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-QNB -12 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-QNB -12 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-QNB -12 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-QNB -12 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
187 253 34 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 253 34 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 253 34 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 253 34 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 253 34 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 253 34 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
135398737 944 89 3H-QNB -10 91 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-QNB -10 91 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-QNB -10 91 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-QNB -10 91 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-QNB -10 91 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398745 2869 108 3H-NMS -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2869 108 3H-QNB -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-NMS -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-QNB -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-NMS -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-QNB -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-NMS -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-QNB -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 944 89 3H-QNB -7 91 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-QNB -7 91 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-QNB -7 91 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-QNB -7 91 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-QNB -7 91 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 2316 44 3H-QNB -58 44 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-QNB -58 44 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-QNB -58 44 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-QNB -58 44 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-QNB -58 44 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2435 3533 78 3H-QNB -5248 48 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-QNB -5248 48 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-QNB -5248 48 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-QNB -5248 48 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-QNB -5248 48 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 3533 78 3H-QNB -239 48 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-QNB -239 48 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-QNB -239 48 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-QNB -239 48 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-QNB -239 48 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
154734599 2467 8 3H-NMS -19 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2467 8 3H-NMS -19 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2467 8 3H-NMS -19 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2467 8 3H-NMS -19 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
108107 79534 30 3H-NMS -4 15 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
156592250 79534 30 3H-NMS -4 15 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL1256878 79534 30 3H-NMS -4 15 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL212579 79534 30 3H-NMS -4 15 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
None 215339 0 UNDEFINED - 1 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 4 1 2 4.8 CC1=C(C=C(C=C1NC2CC2)C3CC3)N4CCCCCC4 None
44431381 148489 0 UNDEFINED -1 3 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 318 6 1 4 2.9 CN(C)C1(CNCCC2CCCC2)COc2ccccc2OC1 None
CHEMBL394254 148489 0 UNDEFINED -1 3 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 318 6 1 4 2.9 CN(C)C1(CNCCC2CCCC2)COc2ccccc2OC1 None
71128 96362 18 3H-NMS -3 8 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 None
CHEMBL26505 96362 18 3H-NMS -3 8 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 None
1734 116 8 3H-NMS -2 12 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 8 3H-NMS -2 12 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 8 3H-NMS -2 12 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
2381 656 43 3H-QNB -9 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
374 656 43 3H-QNB -9 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
7128 656 43 3H-QNB -9 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
CHEMBL1101 656 43 3H-QNB -9 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
DB00810 656 43 3H-QNB -9 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
310 1891 0 3H-NMS 3 11 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
3602 1891 0 3H-NMS 3 11 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
CHEMBL3545990 1891 0 3H-NMS 3 11 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
154734599 2467 8 3H-NMS -66 11 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2467 8 3H-NMS -66 11 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2467 8 3H-NMS -66 11 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2467 8 3H-NMS -66 11 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
154734599 2467 8 3H-PIRENZEPINE -66 11 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2467 8 3H-PIRENZEPINE -66 11 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2467 8 3H-PIRENZEPINE -66 11 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2467 8 3H-PIRENZEPINE -66 11 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
62865 1248 0 3H-4-DAMP -5 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 1248 0 3H-4-DAMP -5 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 1248 0 3H-4-DAMP -5 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 1248 0 3H-4-DAMP -5 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 1248 0 3H-4-DAMP -5 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
2200 3082 38 3H-NMS -22 13 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-NMS -22 13 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-NMS -22 13 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-NMS -22 13 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-NMS -22 13 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
46780481 107045 18 3H-NMS -776 53 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 3H-NMS -776 53 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 3H-NMS -776 53 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 3H-NMS -776 53 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3337 214441 0 3H-QNB -158 40 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214441 0 3H-QNB -158 40 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214441 0 3H-QNB -158 40 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214441 0 3H-QNB -158 40 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
114743 214331 0 3H-QNB -2 8 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 291 1 1 1 4.9 C1CC(C2=CC=CC=C2C1C3=CC(=C(C=C3)Cl)Cl)N None
None 214502 0 3H-NMS -3090 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
20980871 214683 0 3H-QNB -9 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 3 0 2 4.7 CN(C)CCC=C1C2=CC=CC=C2CSC3=CC=CC=C31 None
2774 3807 92 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 3807 92 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 3807 92 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 3807 92 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 3807 92 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 3807 92 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
132947 3803 8 3H-NMS -309 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
361 3803 8 3H-NMS -309 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
CHEMBL265256 3803 8 3H-NMS -309 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
180 397 50 3H-Arachidonic Acid -23 38 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-Arachidonic Acid -23 38 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-Arachidonic Acid -23 38 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-Arachidonic Acid -23 38 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-Arachidonic Acid -23 38 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
3652 4034 72 3H-QNB -3 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4034 72 3H-QNB -3 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4034 72 3H-QNB -3 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4034 72 3H-QNB -3 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4034 72 3H-QNB -3 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
1613 2316 44 3H-QNB -15 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-QNB -15 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-QNB -15 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-QNB -15 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-QNB -15 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2337 3205 72 3H-QNB -257 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-QNB -257 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-QNB -257 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-QNB -257 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-QNB -257 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
10938 1672 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
299 1672 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
3256 1672 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
CHEMBL2110739 1672 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
2370 616 30 None 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
297 616 30 None 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
358 616 30 None 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
CHEMBL1482 616 30 None 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
DB01019 616 30 None 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
44431391 145888 0 UNDEFINED 1 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 352 6 1 5 2.3 CN(C)C1(CNCCC2CCOCC2)COc2ccc(F)cc2OC1 None
CHEMBL392186 145888 0 UNDEFINED 1 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 352 6 1 5 2.3 CN(C)C1(CNCCC2CCOCC2)COc2ccc(F)cc2OC1 None
187 253 34 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 253 34 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 253 34 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 253 34 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 253 34 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 253 34 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
44431380 87557 0 UNDEFINED 2 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 318 5 1 4 2.9 CN(C)C1(CNCC2CCCCC2)COc2ccccc2OC1 None
CHEMBL234257 87557 0 UNDEFINED 2 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 318 5 1 4 2.9 CN(C)C1(CNCC2CCCCC2)COc2ccccc2OC1 None
279 1631 26 3H-QNB -8 17 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1631 26 3H-QNB -8 17 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1631 26 3H-QNB -8 17 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
187 253 34 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 253 34 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 253 34 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 253 34 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 253 34 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 253 34 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
2230 461 55 3H-QNB -588 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
296 461 55 3H-QNB -588 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
CHEMBL7303 461 55 3H-QNB -588 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
DB04365 461 55 3H-QNB -588 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
100 3745 52 3H-QNB -8 55 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-QNB -8 55 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-QNB -8 55 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-QNB -8 55 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-QNB -8 55 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
135398745 2869 108 3H-QNB -16 65 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-QNB -16 65 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-QNB -16 65 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-QNB -16 65 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
7534 214623 0 3H-NMS -4 5 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 291 3 1 4 2.5 CC1CC(CC(N1C)(C)C)OC(=O)C(C2=CC=CC=C2)O None
None 214504 0 3H-NMS -1 5 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 311 3 1 2 3.9 C1CCC(CC1)C(C#CCN2CCCCC2)(C3=CC=CC=C3)O None
2200 3082 38 3H-NMS -22 13 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-NMS -22 13 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-NMS -22 13 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-NMS -22 13 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-NMS -22 13 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
134 2478 19 3H-QNB -134 67 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-QNB -134 67 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-QNB -134 67 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-QNB -134 67 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-QNB -134 67 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
242 467 117 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 467 117 3H-QNB -3388 51 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-QNB -3388 51 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-QNB -3388 51 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-QNB -3388 51 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-QNB -3388 51 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 467 117 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2726 906 64 3H-QNB -18 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-QNB -18 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-QNB -18 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-QNB -18 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-QNB -18 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1192 147 41 3H-NMS -75 16 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1794 147 41 3H-NMS -75 16 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
CHEMBL501701 147 41 3H-NMS -75 16 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1353 1880 85 None -154 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 None -154 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 None -154 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 None -154 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 None -154 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1830 2552 39 None -39 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 None -39 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 None -39 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 None -39 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 None -39 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
2389 3279 114 None -575 67 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 None -575 67 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 None -575 67 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 None -575 67 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 None -575 67 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2865 4079 67 None -812 53 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 None -812 53 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 None -812 53 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 None -812 53 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 None -812 53 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2448 214184 0 None -134 17 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 419 6 1 3 4.5 C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F None
42470 214429 0 3H-NMS -14 6 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 345 10 0 3 4.9 CCN(CCCC(=O)C1CCCCC1)C(C)CC2=CC=C(C=C2)OC None
4066 202920 72 3H-QNB 1 7 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
CHEMBL73451 202920 72 3H-QNB 1 7 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
3652 45983 62 None -1 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
CHEMBL1535 45983 62 None -1 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
242 467 117 None -114 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 None -114 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 None -114 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 None -114 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 None -114 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
66265 93579 12 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 93579 12 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
212 3746 43 None -5 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3746 43 None -5 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3746 43 None -5 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3746 43 None -5 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3746 43 None -5 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
448537 159703 86 None -28 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 159703 86 None -28 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
28417 39799 48 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
CHEMBL1479 39799 48 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
2719 904 66 None -3 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
5535 904 66 None -3 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
607 904 66 None -3 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
CHEMBL76 904 66 None -3 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
DB00608 904 66 None -3 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
441383 20133 54 None -6 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL1306 20133 54 None -6 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
2435 3533 78 None -239 48 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 None -239 48 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 None -239 48 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 None -239 48 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 None -239 48 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2812 4711 96 None -22 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4711 96 None -22 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
16362 3076 67 None -562 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 None -562 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 None -562 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 None -562 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 None -562 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
209 3008 94 None -144 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 None -144 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 None -144 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 None -144 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 None -144 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2337 3205 72 None -81 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 None -81 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 None -81 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 None -81 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 None -81 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
44431388 86891 0 UNDEFINED 2 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 348 6 1 5 2.8 CN(C)C1(CNCCC2=CCSCC2)COc2ccccc2OC1 None
CHEMBL233202 86891 0 UNDEFINED 2 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 348 6 1 5 2.8 CN(C)C1(CNCCC2=CCSCC2)COc2ccccc2OC1 None
3389 215982 0 None -1 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
1836 2554 56 None -42 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
3340 2554 56 None -42 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
5281040 2554 56 None -42 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
CHEMBL787 2554 56 None -42 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
DB00471 2554 56 None -42 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
107782 14330 16 None -1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
67151996 14330 16 None -1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
CHEMBL1201207 14330 16 None -1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
68617 203816 60 None -12 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 203816 60 None -12 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 203816 60 None -12 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
308 2029 20 3H-NMS 1 9 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
3603 2029 20 3H-NMS 1 9 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
CHEMBL1256682 2029 20 3H-NMS 1 9 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
4543 169982 36 3H-QNB -3 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169982 36 3H-QNB -3 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169982 36 3H-QNB -3 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
15897 2817 0 3H-QNB -32 36 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2817 0 3H-QNB -32 36 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2817 0 3H-QNB -32 36 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
135398745 2869 108 3H-QNB -27 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-QNB -27 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-QNB -27 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-QNB -27 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5831 214185 0 3H-NMS -51 12 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
1225 1443 24 3H-QNB -69 21 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1443 24 3H-QNB -69 21 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1443 24 3H-QNB -69 21 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1443 24 3H-QNB -69 21 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1443 24 3H-QNB -69 21 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
6450478 214238 0 3H-QNB -10 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 340 0 0 6 3.4 CN1CCN(CC1)C2=NC3=CSC=C3C(=CC#N)C4=CSC=C42 None
44431372 86887 0 UNDEFINED -1 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 368 7 1 4 3.7 CC(C)c1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 None
CHEMBL233198 86887 0 UNDEFINED -1 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 368 7 1 4 3.7 CC(C)c1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 None
2865 4079 67 3H-QNB -11481 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-QNB -11481 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-QNB -11481 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-QNB -11481 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-QNB -11481 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
73707487 214624 0 3H-NMS -8 9 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 355 3 1 4 2.5 CN1C2CCC1CC(C2)OC(=O)C(C3=CC=CC=C3)O.Br None
1212 1632 45 None -407 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 None -407 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 None -407 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 None -407 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 None -407 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1209 1628 69 None -30 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1628 69 None -30 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1628 69 None -30 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1628 69 None -30 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1628 69 None -30 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
214 3799 52 None -93 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 None -93 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 None -93 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 None -93 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 None -93 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 None -93 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
657255 197406 29 None -11 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
CHEMBL588119 197406 29 None -11 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
5353853 17803 41 None -13 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
9556529 17803 41 None -13 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1262 17803 41 None -13 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
11057 175575 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
3468 175575 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL459265 175575 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL64894 175575 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
5318 15400 44 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1200348 15400 44 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1221 15400 44 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
176 394 63 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 394 63 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 394 63 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 394 63 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 394 63 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
4189 205195 91 None -12 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 205195 91 None -12 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 205195 91 None -12 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
4746 203183 29 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
CHEMBL1334033 203183 29 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
CHEMBL75880 203183 29 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
1016 3690 75 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3690 75 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3690 75 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3690 75 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3690 75 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3690 75 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
1210 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 905 45 None -79 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6918558 216013 0 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)N(CC[C@H](C1=CC=CC=C1)C1=C(OC(=O)C(C)C)C=CC(CO)=C1)C(C)C None
1548955 88153 17 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2800 88153 17 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 88153 17 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2745 3800 39 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3800 39 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3800 39 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3800 39 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3800 39 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3800 39 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
191 399 92 None -37 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 None -37 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 None -37 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 None -37 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 None -37 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
3198 203802 73 None -10 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 203802 73 None -10 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 203802 73 None -10 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
2274 3124 53 None -21 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 None -21 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 None -21 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 None -21 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 None -21 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
12488 1627 51 None -8 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
941361 1627 51 None -8 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
CHEMBL30008 1627 51 None -8 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
DB04841 1627 51 None -8 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
135 2496 38 None -22 57 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 None -22 57 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 None -22 57 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 None -22 57 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 None -22 57 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
237 203157 43 None 1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL546257 203157 43 None 1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL554190 203157 43 None 1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL7568 203157 43 None 1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
1530 2151 44 None -57 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2151 44 None -57 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2151 44 None -57 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2151 44 None -57 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2151 44 None -57 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
2200 3082 38 None -15 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 None -15 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 None -15 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 None -15 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 None -15 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
1224 1404 79 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1404 79 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1404 79 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1404 79 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1404 79 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1404 79 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
2995 202700 49 None -5 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 202700 49 None -5 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 202700 49 None -5 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
21855 83830 35 None -14 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 None
CHEMBL22108 83830 35 None -14 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 None
72064 77994 9 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
Drug Central 318 8 0 4 3.1 CCN(CC)CCOC(=O)C(c1ccccc1)N1CCCCC1 None
CHEMBL2110892 77994 9 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
Drug Central 318 8 0 4 3.1 CCN(CC)CCOC(=O)C(c1ccccc1)N1CCCCC1 None
2247 502 77 None -19 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 502 77 None -19 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 502 77 None -19 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 502 77 None -19 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 502 77 None -19 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1547484 927 70 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 927 70 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 927 70 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 927 70 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 927 70 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
6726 1254 46 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
7151 1254 46 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
749 1254 46 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL648 1254 46 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB01176 1254 46 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
44431387 86890 0 UNDEFINED 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 350 6 1 5 2.9 CN(C)C1(CNCCC2CCSCC2)COc2ccccc2OC1 None
CHEMBL233201 86890 0 UNDEFINED 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 350 6 1 5 2.9 CN(C)C1(CNCCC2CCSCC2)COc2ccccc2OC1 None
3191 102385 93 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102385 93 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
3947 214378 0 None -4 15 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1C2=CC=CC=C2CCC3=CC=CC=C31)CC(=O)C4=CC=C(C=C4)Cl None
1613 2316 44 None -15 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 None -15 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 None -15 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 None -15 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 None -15 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1427 1982 50 3H-QNB -2 26 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1982 50 3H-QNB -2 26 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1982 50 3H-QNB -2 26 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1982 50 3H-QNB -2 26 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1982 50 3H-QNB -2 26 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
2726 906 64 3H-QNB -35 72 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-QNB -35 72 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-QNB -35 72 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-QNB -35 72 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-QNB -35 72 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
129989 447 41 3H-NMS -16 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC None
8584 447 41 3H-NMS -16 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC None
CHEMBL43383 447 41 3H-NMS -16 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC None
None 214506 0 3H-NMS -10 5 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 574 9 3 7 4.0 CCCN(CCC)CC1CCCCN1CCNC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4.CS(=O)(=O)O None
2726 906 64 3H-QNB -18 72 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-QNB -18 72 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-QNB -18 72 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-QNB -18 72 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-QNB -18 72 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
3337 214441 0 3H-QNB -158 40 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214441 0 3H-QNB -158 40 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214441 0 3H-QNB -158 40 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214441 0 3H-QNB -158 40 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
4011 81996 43 None -14 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 81996 43 None -14 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
4976 201885 27 None -1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
CHEMBL668 201885 27 None -1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
135398737 944 89 3H-NMS -10 91 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-QNB -10 91 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-NMS -10 91 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-QNB -10 91 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-NMS -10 91 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-QNB -10 91 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-NMS -10 91 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-QNB -10 91 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-NMS -10 91 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-QNB -10 91 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1712 2456 0 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
2284 3133 27 None -10 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3133 27 None -10 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3133 27 None -10 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3133 27 None -10 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3133 27 None -10 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2335 11743 21 None -1 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
8478 11743 21 None -1 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL1182210 11743 21 None -1 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL221753 11743 21 None -1 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
135398745 2869 108 None -27 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 None -27 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 None -27 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 None -27 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
103 4089 56 None -144 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 None -144 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 None -144 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 None -144 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 None -144 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1427 1982 50 None -2 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1982 50 None -2 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1982 50 None -2 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1982 50 None -2 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1982 50 None -2 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
4919 204511 21 3H-NMS -1 9 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 204511 21 3H-NMS -1 9 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
2726 906 64 None -18 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 None -18 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 None -18 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 None -18 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 None -18 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
3055 1405 43 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
313 1405 43 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
7163 1405 43 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
CHEMBL936 1405 43 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
DB01231 1405 43 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
1225 1443 24 None -69 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1443 24 None -69 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1443 24 None -69 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1443 24 None -69 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1443 24 None -69 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
4543 169982 36 None -3 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169982 36 None -3 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169982 36 None -3 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
6075 149575 36 None -3 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 149575 36 None -3 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
43815 186337 58 None -5 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186337 58 None -5 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186337 58 None -5 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
5284550 215977 0 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC\C=C1/C2=CC=CC=C2CSC2=CC=CC=C12 None
4601 205020 29 None -1 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 205020 29 None -1 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 205020 29 None -1 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
2801 161325 56 None -1 28 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL1200710 161325 56 None -1 28 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL415 161325 56 None -1 28 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
124087 1362 106 None -9 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 1362 106 None -9 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 1362 106 None -9 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 1362 106 None -9 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 1362 106 None -9 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
62865 1248 0 None -5 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 1248 0 None -5 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 1248 0 None -5 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 1248 0 None -5 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 1248 0 None -5 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
2774 3807 92 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 3807 92 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 3807 92 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 3807 92 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 3807 92 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 3807 92 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
2200 3082 38 None -22 13 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 None -22 13 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 None -22 13 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 None -22 13 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 None -22 13 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
135398737 944 89 None -10 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -10 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -10 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -10 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -10 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 3745 52 None -8 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 None -8 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 None -8 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 None -8 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 None -8 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5387 94438 24 3H-NMS -4 6 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O None
CHEMBL253978 94438 24 3H-NMS -4 6 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O None
73707487 214624 0 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 355 3 1 4 2.5 CN1C2CCC1CC(C2)OC(=O)C(C3=CC=CC=C3)O.Br None
3652 4034 72 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4034 72 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4034 72 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4034 72 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4034 72 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
180 397 50 None -23 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 None -23 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 None -23 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 None -23 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 None -23 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
4919 204511 21 None -2 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 204511 21 None -2 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
2337 3205 72 3H-NMS -81 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-NMS -81 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-NMS -81 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-NMS -81 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-NMS -81 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1353 1880 85 3H-QNB -2344 85 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-QNB -2344 85 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-QNB -2344 85 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-QNB -2344 85 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-QNB -2344 85 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2448 214184 0 3H-QNB -5011 17 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F None
2448 214184 0 3H-QNB -134 17 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F None
103 4089 56 3H-QNB -60 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-QNB -60 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-QNB -60 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-QNB -60 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-QNB -60 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2200 3082 38 3H-NMS -22 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-NMS -22 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-NMS -22 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-NMS -22 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-NMS -22 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
103 4089 56 3H-QNB -144 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-QNB -144 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-QNB -144 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-QNB -144 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-QNB -144 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
208 2820 0 3H-QNB -8 12 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
4541 2820 0 3H-QNB -8 12 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL1494 2820 0 3H-QNB -8 12 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
154059 3580 49 None 1 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
2457 3580 49 None 1 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
7483 3580 49 None 1 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
CHEMBL1734 3580 49 None 1 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
DB01591 3580 49 None 1 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
277 1274 55 None -11 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 None -11 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 None -11 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 None -11 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 None -11 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
26987 936 29 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 936 29 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 936 29 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 936 29 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 936 29 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2705 3781 59 None -1 10 Rat 8.1 pKi = 8.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
360 3781 59 None -1 10 Rat 8.1 pKi = 8.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
443879 3781 59 None -1 10 Rat 8.1 pKi = 8.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
CHEMBL1382 3781 59 None -1 10 Rat 8.1 pKi = 8.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
DB01036 3781 59 None -1 10 Rat 8.1 pKi = 8.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
4904 215997 0 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 1 2 3.8 OC(CCN1CCCCC1)(C1=CC=CC=C1)C1=CC=CC=C1 None
5648 78002 7 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 None
CHEMBL2107687 78002 7 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 None
CHEMBL2111176 78002 7 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 None
2286 3134 48 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3134 48 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3134 48 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3134 48 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3134 48 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2705 3781 59 None -1 10 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
360 3781 59 None -1 10 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
443879 3781 59 None -1 10 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
CHEMBL1382 3781 59 None -1 10 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
DB01036 3781 59 None -1 10 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
10470 2453 5 None -11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
Drug Central 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C None
1689 2453 5 None -11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
Drug Central 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C None
4057 2453 5 None -11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
Drug Central 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C None
CHEMBL524004 2453 5 None -11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
Drug Central 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C None
DB04843 2453 5 None -11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
Drug Central 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C None
319 1297 39 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
321 1297 39 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
444031 1297 39 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
784 1297 39 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
CHEMBL1346 1297 39 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
DB00496 1297 39 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
1371 1892 0 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
24199 1892 0 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
323 1892 0 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
CHEMBL1201325 1892 0 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
DB06787 1892 0 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
1201549 590 22 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 590 22 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 590 22 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 590 22 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 590 22 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 590 22 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
43815 186337 58 3H-QNB -5 24 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186337 58 3H-QNB -5 24 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186337 58 3H-QNB -5 24 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
2200 3082 38 3H-NMS -22 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3082 38 3H-NMS -22 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3082 38 3H-NMS -22 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3082 38 3H-NMS -22 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3082 38 3H-NMS -22 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
154825138 214267 0 3H-NMS -30 12 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
2389 3279 114 3H-QNB -21877 67 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-QNB -21877 67 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-QNB -21877 67 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-QNB -21877 67 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-QNB -21877 67 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1712 2456 0 3H-QNB -22 21 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 3H-QNB -22 21 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 3H-QNB -22 21 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 3H-QNB -22 21 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 3H-QNB -22 21 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
2028 2931 77 None -1 11 Rat 8.0 pKi = 8.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2931 77 None -1 11 Rat 8.0 pKi = 8.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2931 77 None -1 11 Rat 8.0 pKi = 8.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2931 77 None -1 11 Rat 8.0 pKi = 8.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2931 77 None -1 11 Rat 8.0 pKi = 8.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
3042 1386 31 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1386 31 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1386 31 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1386 31 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1386 31 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
2028 2931 77 None 1 11 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2931 77 None 1 11 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2931 77 None 1 11 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2931 77 None 1 11 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2931 77 None 1 11 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
123134663 216005 0 None -1 3 Dog 8.0 pKi = 8.0 Binding
radioligand ([3H]QNB) displacement assayradioligand ([3H]QNB) displacement assay
Drug Central 330 2 0 2 5.4 C[N@+]12CCCC[C@@H]1CCC(C2)=C(C1=CC=CS1)C1=CC=CS1 None
25897919 55363 11 None 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
657309 55363 11 None 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL1464005 55363 11 None 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL1621597 55363 11 None 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
11968014 12649 4 None -5 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 None
CHEMBL1187846 12649 4 None -5 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 None
12057539 206301 39 None 1 20 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 None 1 20 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 None 1 20 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
367 3764 8 None -30 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
5487427 3764 8 None -30 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
8592 3764 8 None -30 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL1900528 3764 8 None -30 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL3305968 3764 8 None -30 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL4650755 3764 8 None -30 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
DB01409 3764 8 None -30 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
2784 939 0 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
351 939 0 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
366 939 0 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
676 939 0 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
CHEMBL620 939 0 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
DB00771 939 0 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
11693 1797 12 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
3494 1797 12 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
4302 1797 12 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
7459 1797 12 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
CHEMBL1201335 1797 12 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
DB00986 1797 12 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
25897919 55363 11 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
657309 55363 11 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL1464005 55363 11 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL1621597 55363 11 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
10129 3270 0 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
11753673 3270 0 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
5303 3270 0 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
CHEMBL3833319 3270 0 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
DB11855 3270 0 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
154417 92828 57 None -2 10 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 None
CHEMBL2449003 92828 57 None -2 10 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 None
12057539 206301 39 None -2 20 Rat 8.0 pKi = 8 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 None -2 20 Rat 8.0 pKi = 8 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 None -2 20 Rat 8.0 pKi = 8 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
1712 2456 0 3H-QNB -6 21 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 3H-QNB -6 21 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 3H-QNB -6 21 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 3H-QNB -6 21 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 3H-QNB -6 21 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
154825138 214267 0 3H-NMS -30 12 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
154825138 214267 0 3H-NMS -17 12 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
135409468 2004 63 3H-QNB -32 40 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2004 63 3H-QNB -32 40 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2004 63 3H-QNB -32 40 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
4601 205020 29 3H-NMS -4 17 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 205020 29 3H-NMS -4 17 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 205020 29 3H-NMS -4 17 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
10104 3510 7 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding to hM3 receptors expressed in CHO cells.Binding to hM3 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
6604866 3510 7 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding to hM3 receptors expressed in CHO cells.Binding to hM3 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
CHEMBL1493369 3510 7 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding to hM3 receptors expressed in CHO cells.Binding to hM3 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
10129 3270 0 None 1 5 Human 9.8 pKi = 9.8 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
11753673 3270 0 None 1 5 Human 9.8 pKi = 9.8 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
5303 3270 0 None 1 5 Human 9.8 pKi = 9.8 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
CHEMBL3833319 3270 0 None 1 5 Human 9.8 pKi = 9.8 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
DB11855 3270 0 None 1 5 Human 9.8 pKi = 9.8 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
123603 870 25 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
2684 870 25 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
584 870 25 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
9658 870 25 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
CHEMBL168815 870 25 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
2293 3137 23 None -1 4 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
329 3137 23 None -1 4 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
4934 3137 23 None -1 4 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
CHEMBL1180725 3137 23 None -1 4 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
DB00782 3137 23 None -1 4 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
11434515 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
11434515 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
11519741 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
11519741 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
4484 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
4484 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
7449 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
7449 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
CHEMBL1194325 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
CHEMBL1194325 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
DB08897 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
DB08897 259 3 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
11519069 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
11519069 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
11519070 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
11519070 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
4816 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
4816 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
7354 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
7354 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
CHEMBL1187833 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
CHEMBL1187833 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
DB09076 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
DB09076 3876 2 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
367 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
367 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
367 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
367 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
367 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
5487427 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
5487427 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
5487427 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
5487427 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
5487427 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
8592 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
8592 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
8592 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
8592 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
8592 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
CHEMBL1900528 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
CHEMBL1900528 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
CHEMBL1900528 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
CHEMBL1900528 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
CHEMBL1900528 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
CHEMBL3305968 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
CHEMBL3305968 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
CHEMBL3305968 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
CHEMBL3305968 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
CHEMBL3305968 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
CHEMBL4650755 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
CHEMBL4650755 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
CHEMBL4650755 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
CHEMBL4650755 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
CHEMBL4650755 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
DB01409 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
DB01409 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
DB01409 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
DB01409 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
DB01409 3764 8 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
316 2793 14 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
317 2793 14 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
71183 2793 14 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
CHEMBL3140030 2793 14 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
CHEMBL376897 2793 14 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
DB00462 2793 14 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
2551 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
2551 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
2551 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
298 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
298 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
298 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
488 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
488 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
488 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
CHEMBL965 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
CHEMBL965 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
CHEMBL965 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
DB00411 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
DB00411 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
DB00411 782 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
2370 616 30 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
2370 616 30 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
297 616 30 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
297 616 30 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
358 616 30 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
358 616 30 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
CHEMBL1482 616 30 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
CHEMBL1482 616 30 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
DB01019 616 30 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
DB01019 616 30 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
187 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
187 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
187 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
294 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
294 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
294 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
65 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
65 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
65 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
8593 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
8593 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
8593 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
CHEMBL667 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
CHEMBL667 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
CHEMBL667 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
DB03128 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
DB03128 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
DB03128 253 34 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
303 2930 16 None -89 6 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
4629 2930 16 None -89 6 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
8595 2930 16 None -89 6 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
CHEMBL44674 2930 16 None -89 6 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
2166 3074 46 None -1445 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
2166 3074 46 None -1445 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
305 3074 46 None -1445 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
305 3074 46 None -1445 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
5910 3074 46 None -1445 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
5910 3074 46 None -1445 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
CHEMBL550 3074 46 None -1445 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
CHEMBL550 3074 46 None -1445 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
DB01085 3074 46 None -1445 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
DB01085 3074 46 None -1445 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
302 2929 23 None -309 7 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
302 2929 23 None -309 7 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
4630 2929 23 None -309 7 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
4630 2929 23 None -309 7 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
CHEMBL7634 2929 23 None -309 7 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
CHEMBL7634 2929 23 None -309 7 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
2230 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
2230 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
2230 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
296 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
296 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
296 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
CHEMBL7303 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
CHEMBL7303 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
CHEMBL7303 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
DB04365 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
DB04365 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
DB04365 461 55 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
107867 2927 48 None -16 10 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 2704370
309 2927 48 None -16 10 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 2704370
CHEMBL17045 2927 48 None -16 10 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 2704370
24768606 3967 51 None -50 5 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
3274 3967 51 None -50 5 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
CHEMBL1628667 3967 51 None -50 5 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
129786 1860 0 None -17 4 Rat 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 2 3 5 0.8 NC(=N)N1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 8813552
3276 1860 0 None -17 4 Rat 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 2 3 5 0.8 NC(=N)N1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 8813552
154734599 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
154734599 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
154734599 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
154734599 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
154734599 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
327 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
327 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
327 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
327 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
327 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
4108 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
4108 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
4108 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
4108 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
4108 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
CHEMBL27673 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
CHEMBL27673 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
CHEMBL27673 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
CHEMBL27673 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
CHEMBL27673 2467 8 None -19 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
2200 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
2200 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
2200 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
2200 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2704370
2200 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
2200 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
328 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
328 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
328 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
328 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2704370
328 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
328 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
4848 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
4848 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
4848 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
4848 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2704370
4848 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
4848 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
CHEMBL9967 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
CHEMBL9967 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
CHEMBL9967 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
CHEMBL9967 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2704370
CHEMBL9967 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
CHEMBL9967 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
DB00670 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
DB00670 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
DB00670 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
DB00670 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2704370
DB00670 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
DB00670 3082 38 None -15 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
132947 3803 8 None -309 9 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 18595721
361 3803 8 None -309 9 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 18595721
CHEMBL265256 3803 8 None -309 9 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 18595721
2774 3807 92 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
5593 3807 92 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
7319 3807 92 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
CHEMBL1200604 3807 92 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
DB00809 3807 92 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
DB01199 3807 92 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
324 1894 12 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1331410
324 1894 12 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1994002
324 1894 12 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 7925952
6436265 1894 12 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1331410
6436265 1894 12 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1994002
6436265 1894 12 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 7925952
CHEMBL277642 1894 12 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1331410
CHEMBL277642 1894 12 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1994002
CHEMBL277642 1894 12 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 7925952
119357 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
3264 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
368 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
CHEMBL279453 301 42 None -16 5 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
129989 447 41 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
129989 447 41 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
8584 447 41 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
8584 447 41 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
CHEMBL43383 447 41 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
CHEMBL43383 447 41 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
3652 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
3652 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
3652 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
57 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
57 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
57 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
60809 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
60809 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
CHEMBL21536 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
CHEMBL21536 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
CHEMBL21536 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
DB15357 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
DB15357 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
DB15357 4034 72 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
5282426 1438 0 None -9 6 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
7549 1438 0 None -9 6 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
CHEMBL108947 1438 0 None -9 6 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
154059 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 12122494
154059 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
2457 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 12122494
2457 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
7483 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 12122494
7483 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
CHEMBL1734 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 12122494
CHEMBL1734 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
DB01591 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 12122494
DB01591 3580 49 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
180 397 50 None -23 38 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
200 397 50 None -23 38 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
2160 397 50 None -23 38 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
CHEMBL629 397 50 None -23 38 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
DB00321 397 50 None -23 38 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
129140 3871 0 None -1 4 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 2043926
129140 3871 0 None -1 4 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 9671109
8583 3871 0 None -1 4 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 2043926
8583 3871 0 None -1 4 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 9671109
2705 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
2705 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
360 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
360 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
443879 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
443879 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
CHEMBL1382 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
CHEMBL1382 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
DB01036 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
DB01036 3781 59 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
10470 2453 5 None -11 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 24844758
1689 2453 5 None -11 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 24844758
4057 2453 5 None -11 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 24844758
CHEMBL524004 2453 5 None -11 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 24844758
DB04843 2453 5 None -11 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 24844758
2028 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
2028 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
359 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
359 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
4634 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
4634 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
CHEMBL1231 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
CHEMBL1231 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
DB01062 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
DB01062 2931 77 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
319 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
319 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
319 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
321 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
321 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
321 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
444031 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
444031 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
444031 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
784 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
784 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
784 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
CHEMBL1346 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
CHEMBL1346 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
CHEMBL1346 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
DB00496 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
DB00496 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
DB00496 1297 39 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
3042 1386 31 None -1 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1386 31 None -1 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1386 31 None -1 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1386 31 None -1 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1386 31 None -1 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
174174 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
174174 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
174174 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
174174 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
260 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
260 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
260 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
260 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
320 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
320 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
320 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
320 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
CHEMBL517712 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
CHEMBL517712 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
CHEMBL517712 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
CHEMBL517712 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
DB00572 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
DB00572 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
DB00572 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
DB00572 519 46 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
1734 116 8 None -2 12 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587
307 116 8 None -2 12 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587
CHEMBL168067 116 8 None -2 12 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587
1734 116 8 None 1 12 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
307 116 8 None 1 12 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
CHEMBL168067 116 8 None 1 12 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
3000322 3506 0 None 1 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
3000322 3506 0 None 1 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
330 3506 0 None 1 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
330 3506 0 None 1 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
CHEMBL569713 3506 0 None 1 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
CHEMBL569713 3506 0 None 1 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
DB00747 3506 0 None 1 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
DB00747 3506 0 None 1 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
325 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
325 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 16847442
325 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 19653626
3746 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
3746 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 16847442
3746 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 19653626
657308 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
657308 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 16847442
657308 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 19653626
CHEMBL1615433 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
CHEMBL1615433 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 16847442
CHEMBL1615433 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 19653626
DB00332 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
DB00332 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 16847442
DB00332 2031 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 19653626
2784 939 0 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
351 939 0 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
366 939 0 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
676 939 0 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
CHEMBL620 939 0 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
DB00771 939 0 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
8586 298 0 None 2 4 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 336 5 2 3 1.8 CN(C(=O)C(c1ccccc1)(c1ccccc1)O)C[C@@H]1[C@H]2[C@@H]1CNC2 20590605
9862598 298 0 None 2 4 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 336 5 2 3 1.8 CN(C(=O)C(c1ccccc1)(c1ccccc1)O)C[C@@H]1[C@H]2[C@@H]1CNC2 20590605
42519285 2540 11 None -60 5 Human 4.5 pKi > 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 7 0 6 3.7 CN(C(=O)c1noc(c1)COc1cccc(c1)C(=O)C)[C@H](c1ccccn1)C 24692176
8591 2540 11 None -60 5 Human 4.5 pKi > 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 7 0 6 3.7 CN(C(=O)c1noc(c1)COc1cccc(c1)C(=O)C)[C@H](c1ccccn1)C 24692176
CHEMBL3185781 2540 11 None -60 5 Human 4.5 pKi > 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 7 0 6 3.7 CN(C(=O)c1noc(c1)COc1cccc(c1)C(=O)C)[C@H](c1ccccn1)C 24692176
314 2653 0 None -1122018 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10799315
313 2652 0 None -407 6 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7925952
134 2478 19 None -134 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 None -134 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 None -134 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 None -134 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 None -134 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
46780481 107045 18 None -776 53 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 None -776 53 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 None -776 53 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 None -776 53 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3337 214441 0 None -158 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214441 0 None -158 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214441 0 None -158 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214441 0 None -158 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
3012003 214377 0 None -1 12 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 311 5 0 3 3.8 CN1CCC(C(C1)COC2=CC=C(C=C2)OC)C3=CC=CC=C3 None
11976 907 54 None -12 23 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 None -12 23 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 None -12 23 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 None -12 23 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
2895 201898 35 None -1 8 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
CHEMBL669 201898 35 None -1 8 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
4066 202920 72 None 1 7 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
CHEMBL73451 202920 72 None 1 7 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
10938 1672 0 None -1 4 Human 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
299 1672 0 None -1 4 Human 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
3256 1672 0 None -1 4 Human 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
CHEMBL2110739 1672 0 None -1 4 Human 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
2551 782 23 None -54 11 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
298 782 23 None -54 11 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
488 782 23 None -54 11 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
CHEMBL965 782 23 None -54 11 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
DB00411 782 23 None -54 11 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
300 2474 13 None -3 5 Human 4.6 pKi None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
4141 2474 13 None -3 5 Human 4.6 pKi None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
CHEMBL92387 2474 13 None -3 5 Human 4.6 pKi None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
301 2498 16 None -7 5 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
9571002 2498 16 None -7 5 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
CHEMBL151938 2498 16 None -7 5 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
290 2438 4 None -7 7 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7620715
4022 2438 4 None -7 7 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7620715
5926 2438 4 None -7 7 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7620715
CHEMBL40554 2438 4 None -7 7 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7620715
CHEMBL74300 2438 4 None -7 7 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7620715
187 253 34 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
294 253 34 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
65 253 34 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
8593 253 34 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
CHEMBL667 253 34 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
DB03128 253 34 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
2229 460 17 None -3 5 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
295 460 17 None -3 5 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
CHEMBL128365 460 17 None -3 5 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
22991950 2297 0 None 1 6 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 7 2 2 5.9 OC(C[N+](C)(C)C)CCCC(C1CCC2C1(C)CCC1C2CCC2C1(C)CCC(C2)O)C 12235229
22991950 2297 0 None -1 6 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 7 2 2 5.9 OC(C[N+](C)(C)C)CCCC(C1CCC2C1(C)CCC1C2CCC2C1(C)CCC(C2)O)C 12235229
326 2297 0 None 1 6 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 7 2 2 5.9 OC(C[N+](C)(C)C)CCCC(C1CCC2C1(C)CCC1C2CCC2C1(C)CCC(C2)O)C 12235229
326 2297 0 None -1 6 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 7 2 2 5.9 OC(C[N+](C)(C)C)CCCC(C1CCC2C1(C)CCC1C2CCC2C1(C)CCC(C2)O)C 12235229
107867 2927 48 None -12 10 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
309 2927 48 None -12 10 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
CHEMBL17045 2927 48 None -12 10 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
2200 3082 38 None -22 13 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
328 3082 38 None -22 13 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
4848 3082 38 None -22 13 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
CHEMBL9967 3082 38 None -22 13 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
DB00670 3082 38 None -22 13 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
306 3400 18 None -4 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
3536 3400 18 None -4 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
53930639 3400 18 None -4 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
9577995 3400 18 None -4 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
CHEMBL134641 3400 18 None -4 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
10426487 2798 4 None -2 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
291 2798 4 None -2 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
CHEMBL99521 2798 4 None -2 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
308 2029 20 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
308 2029 20 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
3603 2029 20 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
3603 2029 20 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
CHEMBL1256682 2029 20 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
CHEMBL1256682 2029 20 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
124226 1890 0 None -1 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
322 1890 0 None -1 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
310 1891 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
310 1891 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
3602 1891 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
3602 1891 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
CHEMBL3545990 1891 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
CHEMBL3545990 1891 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
308 2029 20 None 1 9 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 1325587
3603 2029 20 None 1 9 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 1325587
CHEMBL1256682 2029 20 None 1 9 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 1325587
293 2800 0 None -3 5 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1cccc(c1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
9985526 2800 0 None -3 5 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1cccc(c1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
10062394 2998 1 None -3 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
304 2998 1 None -3 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
CHEMBL130715 2998 1 None -3 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
11757797 2799 0 None -63 5 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccc(cc1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
292 2799 0 None -63 5 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccc(cc1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
1371 1892 0 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
24199 1892 0 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
323 1892 0 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
CHEMBL1201325 1892 0 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
DB06787 1892 0 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
130169 3548 0 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O 2704370
331 3548 0 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O 2704370
174174 519 46 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12235229
174174 519 46 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
260 519 46 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12235229
260 519 46 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
320 519 46 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12235229
320 519 46 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
CHEMBL517712 519 46 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12235229
CHEMBL517712 519 46 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
DB00572 519 46 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12235229
DB00572 519 46 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587