Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

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 DOI
10952349 35133 None 0 Human Functional pEC50 = 9.2 9.2 3467 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 564 15 0 10 6.8 CN1CCC=C(c2nsnc2SCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143434 35133 None 0 Human Functional pEC50 = 9.2 9.2 3467 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 564 15 0 10 6.8 CN1CCC=C(c2nsnc2SCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
11072401 30778 None 0 Human Functional pEC50 = 9 9.0 12882 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL139603 30778 None 0 Human Functional pEC50 = 9 9.0 12882 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
9937709 34097 None 0 Human Functional pEC50 = 8.9 8.9 239 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 560 17 0 10 6.2 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL142538 34097 None 0 Human Functional pEC50 = 8.9 8.9 239 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 560 17 0 10 6.2 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
187 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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
187.0 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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
294 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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
65 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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
187 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 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
187.0 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 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
294 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 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
65 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 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 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 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 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 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 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 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
162665337 182276 None 0 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 358 2 2 5 3.1 Cc1c(Cl)nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4783881 182276 None 0 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 358 2 2 5 3.1 Cc1c(Cl)nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
162675795 183416 None 0 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 438 4 2 8 2.9 COc1cc(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.05.026
CHEMBL4798497 183416 None 0 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 438 4 2 8 2.9 COc1cc(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.05.026
137643460 158267 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4088704 158267 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
42598358 16102 None 0 Human Functional pEC50 = 7 7.0 -100 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16102 None 0 Human Functional pEC50 = 7 7.0 -100 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
137656230 159046 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4096878 159046 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
162651352 180309 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 437 3 2 8 2.9 Cc1nc(Cl)c(C)c(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)n1 10.1016/j.bmcl.2019.05.026
CHEMBL4751034 180309 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 437 3 2 8 2.9 Cc1nc(Cl)c(C)c(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)n1 10.1016/j.bmcl.2019.05.026
89445242 174658 None 0 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 308 3 2 4 4.4 Cc1cc(C)c2c(n1)sc1c(NCc3ccccc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4558571 174658 None 0 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 308 3 2 4 4.4 Cc1cc(C)c2c(n1)sc1c(NCc3ccccc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
155518224 170271 None 0 Human Functional pEC50 = 5 5.0 - 1
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 366 4 0 5 3.7 COc1cccnc1C1CCN(C2CCCN(c3cccnc3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4446144 170271 None 0 Human Functional pEC50 = 5 5.0 - 1
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 366 4 0 5 3.7 COc1cccnc1C1CCN(C2CCCN(c3cccnc3)CC2)CC1 10.1021/acsmedchemlett.9b00106
155510640 174034 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 174034 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155510640 174034 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 174034 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
137641943 158478 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4090871 158478 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777104 159123 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4097819 159123 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
53382504 86331 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313395 86331 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
155539719 172873 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4515326 172873 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155564640 175515 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4577985 175515 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
53382504 86331 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313395 86331 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
89768734 164709 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4217300 164709 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
137645408 157909 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
CHEMBL4084306 157909 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
89768734 164709 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4217300 164709 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
127043639 140508 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3810071 140508 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
155539719 172873 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4515326 172873 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155564640 175515 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4577985 175515 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
137635723 156083 None 0 Human Functional pEC50 = 7.0 7.0 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062934 156083 None 0 Human Functional pEC50 = 7.0 7.0 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
5441 2426 None 10 Human Functional pEC50 = 6.0 6.0 -46 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
9893054 2426 None 10 Human Functional pEC50 = 6.0 6.0 -46 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
CHEMBL3616501 2426 None 10 Human Functional pEC50 = 6.0 6.0 -46 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
135126271 164185 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
CHEMBL4210668 164185 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
53382512 86311 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313375 86311 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
53382512 86311 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313375 86311 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
53382528 86328 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313392 86328 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145977993 163568 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203172 163568 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
145977993 163568 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203172 163568 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
135126271 164185 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
CHEMBL4210668 164185 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
145966725 164334 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4212499 164334 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
53382528 86328 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313392 86328 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145966725 164334 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4212499 164334 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137645408 157909 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
CHEMBL4084306 157909 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
145970522 164804 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
CHEMBL4218472 164804 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
145970522 164804 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
CHEMBL4218472 164804 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
78319052 171341 None 0 Human Functional pEC50 = 8.0 8.0 229 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 361 4 0 5 3.3 CCOC(=O)N1CCCC(N2CCC(c3ncccc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4461438 171341 None 0 Human Functional pEC50 = 8.0 8.0 229 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 361 4 0 5 3.3 CCOC(=O)N1CCCC(N2CCC(c3ncccc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
137643460 158267 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4088704 158267 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777143 153842 None 0 Rat Functional pEC50 = 8.0 8.0 5 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3982695 153842 None 0 Rat Functional pEC50 = 8.0 8.0 5 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
89777143 153842 None 0 Rat Functional pEC50 = 8.0 8.0 5 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3982695 153842 None 0 Rat Functional pEC50 = 8.0 8.0 5 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
89777151 158573 None 0 Rat Functional pEC50 = 7.9 7.9 7 2
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4091821 158573 None 0 Rat Functional pEC50 = 7.9 7.9 7 2
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
134207697 174279 None 0 Human Functional pEC50 = 7.0 7.0 10 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 7 3.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5ccc(F)c(F)c5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4549515 174279 None 0 Human Functional pEC50 = 7.0 7.0 10 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 7 3.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5ccc(F)c(F)c5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207701 174640 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 287 2 2 6 1.7 Cc1cc2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4558111 174640 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 287 2 2 6 1.7 Cc1cc2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
9958728 35153 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 532 15 0 10 5.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143468 35153 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 532 15 0 10 5.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
155552432 174168 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3ncns3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4547008 174168 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3ncns3)CC2)CC1 10.1021/acsmedchemlett.9b00106
89445225 170935 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 326 3 2 4 4.5 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(F)cc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4455343 170935 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 326 3 2 4 4.5 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(F)cc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
29262717 140478 None 6 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809603 140478 None 6 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
127043639 140508 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3810071 140508 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
122190994 123604 None 0 Human Functional pEC50 = 6.0 6.0 -21 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 481 4 3 3 5.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)Nc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618436 123604 None 0 Human Functional pEC50 = 6.0 6.0 -21 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 481 4 3 3 5.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)Nc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL5080134 214665 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc(CN4CCOCC4)cc3)ncnc12 10.1016/j.bmcl.2021.128416
43989253 76058 None 2 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 300 3 1 6 2.7 COc1ccc(C)c2sc(NC(=O)c3cnccn3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057394 76058 None 2 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 300 3 1 6 2.7 COc1ccc(C)c2sc(NC(=O)c3cnccn3)nc12 10.1016/j.bmcl.2012.05.109
135126568 164447 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4213855 164447 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
122189499 123337 None 0 Human Functional pEC50 = 7.0 7.0 -4 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 441 3 2 3 4.0 CN1CCCC/C1=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2 10.1016/j.bmcl.2015.08.011
CHEMBL3616504 123337 None 0 Human Functional pEC50 = 7.0 7.0 -4 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 441 3 2 3 4.0 CN1CCCC/C1=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2 10.1016/j.bmcl.2015.08.011
135126568 164447 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4213855 164447 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL5087350 215086 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc4c(c3)COC4)ncnc12 10.1016/j.bmcl.2021.128416
29262717 140478 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809603 140478 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
145973325 164723 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4217458 164723 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
59654579 123607 None 0 Human Functional pEC50 = 6.9 6.9 -5 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618440 123607 None 0 Human Functional pEC50 = 6.9 6.9 -5 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
156017590 177841 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4644084 177841 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
145973325 164723 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4217458 164723 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
162658616 181053 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 439 4 3 9 1.5 Cc1c(CO)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4759565 181053 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 439 4 3 9 1.5 Cc1c(CO)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
127044706 140445 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
CHEMBL3809292 140445 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
134207678 171222 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 3 2 7 2.7 Cc1cc2nncn2c2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4459622 171222 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 3 2 7 2.7 Cc1cc2nncn2c2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c12 10.1016/j.bmcl.2019.06.032
134207707 172327 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4475459 172327 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
24967746 16055 None 0 Human Functional pEC50 = 7.9 7.9 -31 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16055 None 0 Human Functional pEC50 = 7.9 7.9 -31 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
682264 40210 None 15 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 40210 None 15 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
89452242 175437 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 346 3 1 6 4.7 Cc1nc2sc3c(NCc4ccco4)nn(C)c3c2c(C)c1Cl 10.1016/j.bmcl.2018.12.039
CHEMBL4576513 175437 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 346 3 1 6 4.7 Cc1nc2sc3c(NCc4ccco4)nn(C)c3c2c(C)c1Cl 10.1016/j.bmcl.2018.12.039
134207717 171294 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 3.3 Cc1cc2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4460701 171294 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 3.3 Cc1cc2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
134207690 174645 None 0 Human Functional pEC50 = 6.9 6.9 5 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 434 4 2 9 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(C6CC6)nc5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4558206 174645 None 0 Human Functional pEC50 = 6.9 6.9 5 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 434 4 2 9 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(C6CC6)nc5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207705 175908 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.6 Cc1nc2cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4587040 175908 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.6 Cc1nc2cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc3n2n1 10.1016/j.bmcl.2019.06.032
162647361 179681 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 415 4 2 8 2.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ccc(C5CC5)nn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4743571 179681 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 415 4 2 8 2.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ccc(C5CC5)nn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
89452686 170672 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 298 3 2 5 4.0 Cc1cc(C)c2c(n1)sc1c(NCc3ccco3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4451608 170672 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 298 3 2 5 4.0 Cc1cc(C)c2c(n1)sc1c(NCc3ccco3)n[nH]c12 10.1016/j.bmcl.2018.12.039
134207730 173066 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 2 2 5 3.6 Cc1cn2c(cc(C)c3c(N)c(C(=O)NC4Cc5ccccc5C4)sc32)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4519541 173066 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 2 2 5 3.6 Cc1cn2c(cc(C)c3c(N)c(C(=O)NC4Cc5ccccc5C4)sc32)n1 10.1016/j.bmcl.2019.06.032
127044706 140445 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
CHEMBL3809292 140445 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
16309462 26188 None 4 Human Functional pEC50 = 5.9 5.9 -4 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1357034 26188 None 4 Human Functional pEC50 = 5.9 5.9 -4 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
53382518 86312 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313376 86312 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
155543990 173321 None 0 Rat Functional pEC50 = 5.9 5.9 -4 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 402 5 1 7 4.0 Nc1c(C(=O)c2ccncc2)sc2nc(OCc3ccncc3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4526419 173321 None 0 Rat Functional pEC50 = 5.9 5.9 -4 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 402 5 1 7 4.0 Nc1c(C(=O)c2ccncc2)sc2nc(OCc3ccncc3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
45501061 156775 None 12 Human Functional pEC50 = 5.9 5.9 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4070787 156775 None 12 Human Functional pEC50 = 5.9 5.9 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
137641943 158478 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4090871 158478 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
53382518 86312 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313376 86312 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL5087948 215130 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NC3CCCC3)nccc12 10.1016/j.bmcl.2021.128416
156011081 177069 None 0 Human Functional pEC50 = 6.9 6.9 -3 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.8 Cc1c2c(N)c(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632962 177069 None 0 Human Functional pEC50 = 6.9 6.9 -3 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.8 Cc1c2c(N)c(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
25199525 16081 None 0 Human Functional pEC50 = 6.9 6.9 -5 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223807 16081 None 0 Human Functional pEC50 = 6.9 6.9 -5 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
137659901 159545 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
CHEMBL4102480 159545 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
53382505 86320 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313384 86320 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382505 86320 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313384 86320 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137654582 159004 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4096463 159004 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
56592910 76057 None 1 Human Functional pEC50 = 5.9 5.9 -5 2
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057392 76057 None 1 Human Functional pEC50 = 5.9 5.9 -5 2
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2012.05.109
137659901 159545 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
CHEMBL4102480 159545 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
137654582 159004 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4096463 159004 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
71533671 112025 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 450 4 0 6 2.5 CCOC(=O)N1CCC(C)(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
CHEMBL3289442 112025 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 450 4 0 6 2.5 CCOC(=O)N1CCC(C)(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
89777151 158573 None 0 Rat Functional pEC50 = 7.9 7.9 7 2
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4091821 158573 None 0 Rat Functional pEC50 = 7.9 7.9 7 2
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
134207699 175378 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 286 2 2 5 2.3 Cc1cc2nccn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4574990 175378 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 286 2 2 5 2.3 Cc1cc2nccn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
734373 15279 None 23 Rat Functional pEC50 = 5.9 5.9 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 311 3 2 4 3.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3)sc2n1 10.1038/nchembio.2007.55
CHEMBL1212983 15279 None 23 Rat Functional pEC50 = 5.9 5.9 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 311 3 2 4 3.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3)sc2n1 10.1038/nchembio.2007.55
137650228 157267 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4076732 157267 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
156022087 178196 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.7 Cc1nc2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4649459 178196 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.7 Cc1nc2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
2159295 76055 None 11 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 288 3 1 5 3.5 COc1ccc(C)c2sc(NC(=O)c3ccco3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057376 76055 None 11 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 288 3 1 5 3.5 COc1ccc(C)c2sc(NC(=O)c3ccco3)nc12 10.1016/j.bmcl.2012.05.109
122191004 123333 None 0 Human Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616497 123333 None 0 Human Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
156016090 177684 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.5 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4641848 177684 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.5 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
53382500 86319 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313383 86319 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
44448421 12337 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
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 12337 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
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 12337 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
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
682264 40210 None 15 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 40210 None 15 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
89777181 144133 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3903798 144133 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
53382500 86319 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313383 86319 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156019946 177982 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)n(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4646110 177982 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)n(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
89777181 144133 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3903798 144133 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
302 2977 None 25 Human Functional pEC50 = 7.9 7.9 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
4630 2977 None 25 Human Functional pEC50 = 7.9 7.9 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
CHEMBL7634 2977 None 25 Human Functional pEC50 = 7.9 7.9 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
129277684 163551 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 363 3 2 5 2.6 Cc1cc2c(nc1N1CCC(Oc3ccc4[nH]ncc4c3)CC1)CNC2=O 10.1021/acsmedchemlett.8b00330
CHEMBL4202966 163551 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 363 3 2 5 2.6 Cc1cc2c(nc1N1CCC(Oc3ccc4[nH]ncc4c3)CC1)CNC2=O 10.1021/acsmedchemlett.8b00330
135154616 164576 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 349 3 0 6 3.0 Cc1cc2c(nc1N1CCC(Oc3cccc(C#N)c3)CC1)COC2=O 10.1021/acsmedchemlett.8b00330
CHEMBL4215436 164576 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 349 3 0 6 3.0 Cc1cc2c(nc1N1CCC(Oc3cccc(C#N)c3)CC1)COC2=O 10.1021/acsmedchemlett.8b00330
134207682 173644 None 0 Human Functional pEC50 = 6.9 6.9 4 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 461 3 2 8 3.5 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cc(Cl)ncc5Cl)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4534301 173644 None 0 Human Functional pEC50 = 6.9 6.9 4 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 461 3 2 8 3.5 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cc(Cl)ncc5Cl)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207728 174687 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 9 2.2 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(Cl)cn5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4559283 174687 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 9 2.2 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(Cl)cn5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
162659751 181294 None 0 Human Functional pEC50 = 6.9 6.9 2 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 409 3 2 8 2.3 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cnc(Cl)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4762280 181294 None 0 Human Functional pEC50 = 6.9 6.9 2 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 409 3 2 8 2.3 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cnc(Cl)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL5089790 215227 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3cnc(C)nc3)ncnc12 10.1016/j.bmcl.2021.128416
137650228 157267 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4076732 157267 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
53382493 86310 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313374 86310 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53002540 159413 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4100855 159413 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
53382493 86310 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313374 86310 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53002540 159413 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4100855 159413 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
156016031 177626 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)nn(C)c4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4641135 177626 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)nn(C)c4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
89777316 157885 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4084063 157885 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5077997 214526 None 1 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(N3CC4(COC4)C3)ncnc12 10.1016/j.bmcl.2021.128416
682264 40210 None 15 Rat Functional pEC50 = 6.8 6.8 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 40210 None 15 Rat Functional pEC50 = 6.8 6.8 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
89777316 157885 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4084063 157885 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
155539604 172844 None 0 Rat Functional pEC50 = 5.8 5.8 -2 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4514671 172844 None 0 Rat Functional pEC50 = 5.8 5.8 -2 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
145972844 164676 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216874 164676 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
155539604 172844 None 0 Rat Functional pEC50 = 5.8 5.8 -2 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4514671 172844 None 0 Rat Functional pEC50 = 5.8 5.8 -2 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
156012013 177367 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 3 2 6 2.1 Cc1c2c(N)c(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4637785 177367 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 3 2 6 2.1 Cc1c2c(N)c(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
145972844 164676 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216874 164676 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
137653138 158920 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4095560 158920 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
53382529 86338 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313404 86338 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137653138 158920 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4095560 158920 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
53382529 86338 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313404 86338 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156013272 177483 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 4 2 7 2.1 COc1cc(N2CC(NC(=O)c3ccc4nn(C)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4639222 177483 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 4 2 7 2.1 COc1cc(N2CC(NC(=O)c3ccc4nn(C)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
156014779 177534 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 339 3 1 5 3.7 Cc1c2c(ccc3c(NCc4ccc(F)c(F)c4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4640119 177534 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 339 3 1 5 3.7 Cc1c2c(ccc3c(NCc4ccc(F)c(F)c4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL5088165 215142 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)oc1c(NC3CN(c4cc(Cl)ncc4Cl)C3)ncnc12 10.1016/j.bmcl.2021.128416
156014138 177242 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 9 2.3 COc1cc(N2CC(Nc3ncnc4c3ccc3nnn(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4635779 177242 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 9 2.3 COc1cc(N2CC(Nc3ncnc4c3ccc3nnn(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
71528087 87585 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 385 4 0 4 2.9 CCOC(=O)N1CCC(C)(CN2CC[C@H](N3C(=O)Cc4ccccc43)C2)CC1 10.1021/ml300372f
CHEMBL2336056 87585 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 385 4 0 4 2.9 CCOC(=O)N1CCC(C)(CN2CC[C@H](N3C(=O)Cc4ccccc43)C2)CC1 10.1021/ml300372f
145966439 164268 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 418 4 1 8 2.3 COc1ccc(OC2CCN(c3nc4oc(=O)[nH]c(=O)c4c(Cl)c3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4211671 164268 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 418 4 1 8 2.3 COc1ccc(OC2CCN(c3nc4oc(=O)[nH]c(=O)c4c(Cl)c3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
137656783 159684 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104144 159684 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
162657433 181163 None 0 Human Functional pEC50 = 6.8 6.8 5 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 428 4 2 7 3.4 Cc1cc(C2CC2)ncc1N1CC(NC(=O)c2sc3nnc(Cl)c(C)c3c2N)C1 10.1016/j.bmcl.2019.05.026
CHEMBL4760902 181163 None 0 Human Functional pEC50 = 6.8 6.8 5 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 428 4 2 7 3.4 Cc1cc(C2CC2)ncc1N1CC(NC(=O)c2sc3nnc(Cl)c(C)c3c2N)C1 10.1016/j.bmcl.2019.05.026
162663713 181968 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 459 4 2 8 2.9 Cc1c(C(F)F)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4780059 181968 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 459 4 2 8 2.9 Cc1c(C(F)F)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL5079861 214649 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NC3CN(c4ncc(C(F)(F)F)cn4)C3)nccc12 10.1016/j.bmcl.2021.128416
683024 51306 None 24 Rat Functional pEC50 = 5.8 5.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL1581020 51306 None 24 Rat Functional pEC50 = 5.8 5.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
117916889 170475 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 4 1 4 4.9 CSc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2C)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4448985 170475 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 4 1 4 4.9 CSc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2C)cc1 10.1016/j.bmcl.2018.12.039
117910878 174408 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 345 4 1 5 3.4 COc1ccc(CNC(=O)c2cc3c(C)c(C)nnc3s2)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL4552552 174408 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 345 4 1 5 3.4 COc1ccc(CNC(=O)c2cc3c(C)c(C)nnc3s2)cc1F 10.1016/j.bmcl.2018.12.039
145966183 164240 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211252 164240 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145966183 164240 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211252 164240 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145964807 164283 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211897 164283 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
683024 51306 None 24 Rat Functional pEC50 = 5.8 5.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL1581020 51306 None 24 Rat Functional pEC50 = 5.8 5.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
145964807 164283 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211897 164283 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL5085861 214995 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(C3CCOCC3)ncnc12 10.1016/j.bmcl.2021.128416
53382480 86329 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313393 86329 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
1505737 86330 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313394 86330 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137632847 156438 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4066953 156438 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5090162 215246 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc(-n4ccnc4)nc3)ncnc12 10.1016/j.bmcl.2021.128416
156013904 177239 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 395 3 2 7 2.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4635732 177239 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 395 3 2 7 2.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
42599068 16079 None 0 Human Functional pEC50 = 6.8 6.8 -50 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16079 None 0 Human Functional pEC50 = 6.8 6.8 -50 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
42598360 16104 None 0 Human Functional pEC50 = 6.8 6.8 -63 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16104 None 0 Human Functional pEC50 = 6.8 6.8 -63 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
137649420 157521 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4079904 157521 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
42598359 16106 None 0 Human Functional pEC50 = 5.8 5.8 -125 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16106 None 0 Human Functional pEC50 = 5.8 5.8 -125 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
42598586 16123 None 0 Human Functional pEC50 = 5.8 5.8 -7 4
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16123 None 0 Human Functional pEC50 = 5.8 5.8 -7 4
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
89777262 156678 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4069641 156678 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
25162692 53682 None 5 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1603219 53682 None 5 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
137656230 159046 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4096878 159046 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5088899 215185 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)oc1c(NC3CCC3)ncnc12 10.1016/j.bmcl.2021.128416
155524827 170917 None 0 Human Functional pEC50 = 7.8 7.8 12 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 4 0 6 3.1 COc1cccnc1C1CCN(C2CCCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4455058 170917 None 0 Human Functional pEC50 = 7.8 7.8 12 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 4 0 6 3.1 COc1cccnc1C1CCN(C2CCCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
134207713 170320 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 321 2 2 6 2.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4446894 170320 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 321 2 2 6 2.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
137656783 159684 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104144 159684 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137646286 157817 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4083327 157817 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
155557669 174662 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 419 4 1 8 3.4 Cc1nnc2sc3c(NCc4ccc(S(C)(=O)=O)c(F)c4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4558665 174662 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 419 4 1 8 3.4 Cc1nnc2sc3c(NCc4ccc(S(C)(=O)=O)c(F)c4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
134207694 170300 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 399 4 2 7 3.2 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nc(C)nn43)c2N)cc1F 10.1016/j.bmcl.2019.06.032
CHEMBL4446559 170300 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 399 4 2 7 3.2 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nc(C)nn43)c2N)cc1F 10.1016/j.bmcl.2019.06.032
134207702 172360 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 442 3 2 9 2.5 Cc1nc(Cl)cc(N2CC(NC(=O)c3sc4c(c(C)cc5nc(C)nn54)c3N)C2)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4475984 172360 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 442 3 2 9 2.5 Cc1nc(Cl)cc(N2CC(NC(=O)c3sc4c(c(C)cc5nc(C)nn54)c3N)C2)n1 10.1016/j.bmcl.2019.06.032
53382480 86329 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313393 86329 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
1505737 86330 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313394 86330 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
16309462 26188 None 4 Rat Functional pEC50 = 6.8 6.8 4 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1357034 26188 None 4 Rat Functional pEC50 = 6.8 6.8 4 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
25162692 53682 None 5 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1603219 53682 None 5 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL5082166 214790 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None COc1ccc(C2CC2Nc2ncnc3c2sc2nc(C)cc(C)c23)cc1 10.1016/j.bmcl.2021.128416
155510640 174034 None 0 Rat Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 174034 None 0 Rat Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
137647620 157598 None 0 Human Functional pEC50 = 6.8 6.8 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4080878 157598 None 0 Human Functional pEC50 = 6.8 6.8 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
89777262 156678 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4069641 156678 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137646601 158002 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4085378 158002 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
155510640 174034 None 0 Rat Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 174034 None 0 Rat Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
137640564 157043 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4073827 157043 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
26441386 140371 None 2 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808425 140371 None 2 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
134207723 175386 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4575270 175386 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
137646286 157817 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4083327 157817 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
129277689 164019 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 395 3 1 6 2.5 Cc1cc2c(nc1N1CC[C@@H](Oc3ccc4c(cnn4C)c3)[C@@H](F)C1)CNC2=O 10.1021/acsmedchemlett.8b00330
CHEMBL4208543 164019 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 395 3 1 6 2.5 Cc1cc2c(nc1N1CC[C@@H](Oc3ccc4c(cnn4C)c3)[C@@H](F)C1)CNC2=O 10.1021/acsmedchemlett.8b00330
12301 4047 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
73774630 4047 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 4047 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
89768534 151634 None 0 Rat Functional pEC50 = 7.8 7.8 14 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3963788 151634 None 0 Rat Functional pEC50 = 7.8 7.8 14 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
12301 4047 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
73774630 4047 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 4047 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
89768534 151634 None 0 Rat Functional pEC50 = 7.8 7.8 14 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3963788 151634 None 0 Rat Functional pEC50 = 7.8 7.8 14 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
162644740 179425 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 441 4 2 8 2.5 Cc1c(CF)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4740272 179425 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 441 4 2 8 2.5 Cc1c(CF)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
26441386 140371 None 2 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808425 140371 None 2 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
137632847 156438 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4066953 156438 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
156020948 178117 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 4 2 7 2.8 Cn1nnc2ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL4648135 178117 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 4 2 7 2.8 Cn1nnc2ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL5082904 214831 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(N3CCC3)ncnc12 10.1016/j.bmcl.2021.128416
156020141 178056 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 2 8 0.4 Cn1nnc2ccc(C(=O)NC3CN(c4ccc(C#N)cn4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4647288 178056 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 2 8 0.4 Cn1nnc2ccc(C(=O)NC3CN(c4ccc(C#N)cn4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
127043636 140486 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809693 140486 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
53382478 86334 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313398 86334 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382478 86334 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313398 86334 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137646601 158002 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4085378 158002 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
89777147 156379 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4066301 156379 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777355 164622 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216038 164622 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
1506223 86332 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313396 86332 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89777355 164622 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216038 164622 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89777147 156379 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4066301 156379 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
3652 4097 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
57 4097 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
60809 4097 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
60809.0 4097 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
CHEMBL21536 4097 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
DB15357 4097 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
135154300 163962 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 461 6 1 8 2.9 Cc1cc(C(=O)NCc2ccncc2)nnc1N1CCC(Oc2ccc3c(c2)OCCO3)CC1 10.1021/acsmedchemlett.8b00330
CHEMBL4207853 163962 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 461 6 1 8 2.9 Cc1cc(C(=O)NCc2ccncc2)nnc1N1CCC(Oc2ccc3c(c2)OCCO3)CC1 10.1021/acsmedchemlett.8b00330
135171475 163981 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 383 4 2 7 1.4 COc1ccc(OC2CCN(c3nc4[nH]c(=O)[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4208024 163981 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 383 4 2 7 1.4 COc1ccc(OC2CCN(c3nc4[nH]c(=O)[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
135171550 164170 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 328 4 1 5 2.4 Cc1cc2c(=O)[nH]ncc2nc1N1CCC(OCC2(C)CC2)CC1 10.1021/acsmedchemlett.8b00330
CHEMBL4210497 164170 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 328 4 1 5 2.4 Cc1cc2c(=O)[nH]ncc2nc1N1CCC(OCC2(C)CC2)CC1 10.1021/acsmedchemlett.8b00330
137658662 159430 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4101054 159430 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137635043 156030 None 13 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062319 156030 None 13 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
155522181 170688 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 317 3 1 7 2.8 Cc1nnc2sc3c(NCC4CCCO4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4451787 170688 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 317 3 1 7 2.8 Cc1nnc2sc3c(NCC4CCCO4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
162650513 180049 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 483 7 2 10 2.0 COCCOc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4747706 180049 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 483 7 2 10 2.0 COCCOc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
1506223 86332 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313396 86332 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
127043636 140486 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809693 140486 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
155540233 172905 None 0 Rat Functional pEC50 = 6.7 6.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4516136 172905 None 0 Rat Functional pEC50 = 6.7 6.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
89768749 159292 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4099560 159292 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
5204148 33995 None 12 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 306 3 1 6 2.4 COc1ccc(C)c2sc(NC(=O)C3=COCCO3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL1424504 33995 None 12 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 306 3 1 6 2.4 COc1ccc(C)c2sc(NC(=O)C3=COCCO3)nc12 10.1016/j.bmcl.2012.05.109
155540233 172905 None 0 Rat Functional pEC50 = 6.7 6.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4516136 172905 None 0 Rat Functional pEC50 = 6.7 6.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
45142487 25951 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cc(F)ccc3F)c(N)c12 nan
CHEMBL1354105 25951 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cc(F)ccc3F)c(N)c12 nan
156017839 177860 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cnc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4644300 177860 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cnc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
137649420 157521 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4079904 157521 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137640564 157043 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4073827 157043 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
127043450 140396 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808696 140396 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
89768749 159292 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4099560 159292 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137635043 156030 None 13 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062319 156030 None 13 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
44253016 80457 None 2 Human Functional pEC50 = 7.7 7.7 -1 4
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit 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 80457 None 2 Human Functional pEC50 = 7.7 7.7 -1 4
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit 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
134207681 175658 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 483 4 2 8 3.4 Cc1nc2cc(C)c3c(N)c(C(=O)NCc4ccc(S(=O)(=O)C(F)(F)F)cc4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4581412 175658 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 483 4 2 8 3.4 Cc1nc2cc(C)c3c(N)c(C(=O)NCc4ccc(S(=O)(=O)C(F)(F)F)cc4)sc3n2n1 10.1016/j.bmcl.2019.06.032
127043450 140396 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808696 140396 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
45142483 52634 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 392 5 2 7 2.4 Cc1cc(OCCN2CCOCC2)nc2sc(C(=O)NC(C)(C)C)c(N)c12 nan
CHEMBL1593296 52634 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 392 5 2 7 2.4 Cc1cc(OCCN2CCOCC2)nc2sc(C(=O)NC(C)(C)C)c(N)c12 nan
155563393 175323 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4573723 175323 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
155563393 175323 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4573723 175323 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
137647620 157598 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4080878 157598 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
42598828 16103 None 0 Human Functional pEC50 = 6.7 6.7 -158 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16103 None 0 Human Functional pEC50 = 6.7 6.7 -158 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
25230693 16125 None 0 Human Functional pEC50 = 6.7 6.7 -79 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16125 None 0 Human Functional pEC50 = 6.7 6.7 -79 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
16038385 80458 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 301 2 1 4 2.1 O=c1[nH]c2ccccc2n1C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL2146598 80458 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 301 2 1 4 2.1 O=c1[nH]c2ccccc2n1C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
145978398 163959 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4207811 163959 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
53382534 86337 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 2 2 5 2.3 Cc1nc2sc(C(=O)NC3COC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313403 86337 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 2 2 5 2.3 Cc1nc2sc(C(=O)NC3COC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
155519300 170372 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3cnsn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4447724 170372 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3cnsn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
134207721 169810 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.9 Cc1c(Cl)c2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4439440 169810 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.9 Cc1c(Cl)c2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
162643836 181716 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 476 3 2 7 3.9 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cc(C(F)(F)F)ncc4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4776981 181716 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 476 3 2 7 3.9 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cc(C(F)(F)F)ncc4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
162661731 181864 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 354 3 2 6 2.5 COc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4778766 181864 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 354 3 2 6 2.5 COc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
162664667 182156 None 0 Human Functional pEC50 = 7.7 7.7 54 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 374 3 2 7 2.2 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4782416 182156 None 0 Human Functional pEC50 = 7.7 7.7 54 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 374 3 2 7 2.2 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
162665586 182395 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 338 2 2 5 2.8 Cc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4785432 182395 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 338 2 2 5 2.8 Cc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
135154593 163609 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 367 3 1 7 1.8 Cc1cn2c(=O)[nH]nc2nc1N1CCC(Oc2ccc3c(c2)COC3)CC1 10.1021/acsmedchemlett.8b00330
CHEMBL4203670 163609 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 367 3 1 7 1.8 Cc1cn2c(=O)[nH]nc2nc1N1CCC(Oc2ccc3c(c2)COC3)CC1 10.1021/acsmedchemlett.8b00330
135150478 163917 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 391 4 2 6 2.8 Cc1c(Cl)nc(CO)nc1N1CC[C@@H](Oc2ccc3[nH]ncc3c2)[C@@H](F)C1 10.1021/acsmedchemlett.8b00330
CHEMBL4207315 163917 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 391 4 2 6 2.8 Cc1c(Cl)nc(CO)nc1N1CC[C@@H](Oc2ccc3[nH]ncc3c2)[C@@H](F)C1 10.1021/acsmedchemlett.8b00330
135150406 164304 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 387 4 0 5 2.7 Cc1cc2c(nc1N1CCC(Oc3ccccc3)CC1)CN(S(C)(=O)=O)C2 10.1021/acsmedchemlett.8b00330
CHEMBL4212205 164304 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 387 4 0 5 2.7 Cc1cc2c(nc1N1CCC(Oc3ccccc3)CC1)CN(S(C)(=O)=O)C2 10.1021/acsmedchemlett.8b00330
145978398 163959 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4207811 163959 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89445258 174707 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 272 3 2 4 3.6 Cc1cc(C)c2c(n1)sc1c(NCC3CC3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4559841 174707 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 272 3 2 4 3.6 Cc1cc(C)c2c(n1)sc1c(NCC3CC3)n[nH]c12 10.1016/j.bmcl.2018.12.039
134207685 170066 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 2 2 5 4.2 Cc1cn2c(cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc32)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4443127 170066 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 2 2 5 4.2 Cc1cn2c(cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc32)n1 10.1016/j.bmcl.2019.06.032
9936450 35155 None 0 Human Functional pEC50 = 4.7 4.7 -27 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143469 35155 None 0 Human Functional pEC50 = 4.7 4.7 -27 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
53382534 86337 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 2 2 5 2.3 Cc1nc2sc(C(=O)NC3COC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313403 86337 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 2 2 5 2.3 Cc1nc2sc(C(=O)NC3COC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL5078186 214541 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(N(C)C)nccc12 10.1016/j.bmcl.2021.128416
137642025 158133 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4087127 158133 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
137642025 158133 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4087127 158133 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
53382508 86316 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313380 86316 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137632597 156325 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(F)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4065706 156325 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(F)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
89768736 144289 None 0 Human Functional pEC50 = 6.7 6.7 -11 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 144289 None 0 Human Functional pEC50 = 6.7 6.7 -11 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
53382508 86316 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313380 86316 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89768736 144289 None 0 Rat Functional pEC50 = 7.7 7.7 11 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 144289 None 0 Rat Functional pEC50 = 7.7 7.7 11 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89768736 144289 None 0 Rat Functional pEC50 = 7.7 7.7 11 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 144289 None 0 Rat Functional pEC50 = 7.7 7.7 11 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
117917124 170792 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 359 4 1 5 3.7 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2C)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL4453085 170792 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 359 4 1 5 3.7 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2C)cc1F 10.1016/j.bmcl.2018.12.039
41358726 171791 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 5 3.9 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc4c(c3)OCCO4)sc2n1 10.1016/j.bmcl.2018.12.039
CHEMBL4467950 171791 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 5 3.9 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc4c(c3)OCCO4)sc2n1 10.1016/j.bmcl.2018.12.039
134207706 174438 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 2 2 5 3.9 Cc1cc2nccn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4553231 174438 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 2 2 5 3.9 Cc1cc2nccn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
137646437 157637 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4081305 157637 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137641641 158318 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 4 2 7 3.6 Cc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
CHEMBL4089170 158318 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 4 2 7 3.6 Cc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
137656749 159610 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 337 3 0 4 4.1 Cc1ccc(OC2CCN(c3ccnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4103287 159610 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 337 3 0 4 4.1 Cc1ccc(OC2CCN(c3ccnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
306 3456 None 21 Human Functional pEC50 = 6.7 6.7 1 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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 3456 None 21 Human Functional pEC50 = 6.7 6.7 1 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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 3456 None 21 Human Functional pEC50 = 6.7 6.7 1 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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 3456 None 21 Human Functional pEC50 = 6.7 6.7 1 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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 3456 None 21 Human Functional pEC50 = 6.7 6.7 1 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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
650899 54414 None 11 Rat Functional pEC50 = 4.7 4.7 -7 5
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1535797 54414 None 11 Rat Functional pEC50 = 4.7 4.7 -7 5
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1609153 54414 None 11 Rat Functional pEC50 = 4.7 4.7 -7 5
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
89777237 156315 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4065565 156315 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777237 156315 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4065565 156315 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
134207726 175074 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 335 2 2 6 2.7 Cc1c(Cl)c2nnc(C)n2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4568327 175074 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 335 2 2 6 2.7 Cc1c(Cl)c2nnc(C)n2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
135153778 164374 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 367 4 1 7 2.1 COc1ccc(OC2CCN(c3nc4cn[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4212929 164374 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 367 4 1 7 2.1 COc1ccc(OC2CCN(c3nc4cn[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
89777060 157121 None 0 Human Functional pEC50 = 7.7 7.7 114 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4074908 157121 None 0 Human Functional pEC50 = 7.7 7.7 114 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777160 153964 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3983700 153964 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777160 153964 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3983700 153964 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
155562860 175186 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 364 2 2 7 2.1 Cc1cc2nncn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4570659 175186 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 364 2 2 7 2.1 Cc1cc2nncn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
162650410 180094 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 400 3 2 9 1.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ncncc4C#N)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4748261 180094 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 400 3 2 9 1.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ncncc4C#N)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
89445250 171167 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 4 2 5 4.4 COc1ccc(CNc2n[nH]c3c2sc2nc(C)cc(C)c23)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4458842 171167 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 4 2 5 4.4 COc1ccc(CNc2n[nH]c3c2sc2nc(C)cc(C)c23)cc1 10.1016/j.bmcl.2018.12.039
155540893 172962 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 5 3.9 CCc1c(C(=O)NCc2ccc(OC)c(F)c2)sc2nnc(C)c(C)c12 10.1016/j.bmcl.2018.12.039
CHEMBL4517529 172962 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 5 3.9 CCc1c(C(=O)NCc2ccc(OC)c(F)c2)sc2nnc(C)c(C)c12 10.1016/j.bmcl.2018.12.039
137656749 159610 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 337 3 0 4 4.1 Cc1ccc(OC2CCN(c3ccnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4103287 159610 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 337 3 0 4 4.1 Cc1ccc(OC2CCN(c3ccnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
137632597 156325 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(F)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4065706 156325 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(F)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
1505736 86292 None 11 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 337 2 2 4 4.2 Cc1nc2sc(C(=O)NC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313073 86292 None 11 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 337 2 2 4 4.2 Cc1nc2sc(C(=O)NC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
135126266 164217 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)nc(Cl)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4210986 164217 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)nc(Cl)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
155544229 173372 None 0 Rat Functional pEC50 = 5.7 5.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4527640 173372 None 0 Rat Functional pEC50 = 5.7 5.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
89777224 164053 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 2 1 6 2.6 Cc1nnc2sc(C(=O)N3CC(F)(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4209023 164053 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 2 1 6 2.6 Cc1nnc2sc(C(=O)N3CC(F)(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
155544229 173372 None 0 Rat Functional pEC50 = 5.7 5.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4527640 173372 None 0 Rat Functional pEC50 = 5.7 5.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
89777224 164053 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 2 1 6 2.6 Cc1nnc2sc(C(=O)N3CC(F)(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4209023 164053 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 2 1 6 2.6 Cc1nnc2sc(C(=O)N3CC(F)(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
11536903 2397 None 68 Rat Functional pEC50 = 6.7 6.7 28 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1016/j.bmcl.2017.10.016
3262 2397 None 68 Rat Functional pEC50 = 6.7 6.7 28 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1016/j.bmcl.2017.10.016
CHEMBL3770346 2397 None 68 Rat Functional pEC50 = 6.7 6.7 28 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1016/j.bmcl.2017.10.016
3263 4025 None 58 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2017.10.016
864492 4025 None 58 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2017.10.016
CHEMBL1978713 4025 None 58 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2017.10.016
12301 4047 None 30 Rat Functional pEC50 = 6.7 6.7 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.016
73774630 4047 None 30 Rat Functional pEC50 = 6.7 6.7 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.016
CHEMBL3915634 4047 None 30 Rat Functional pEC50 = 6.7 6.7 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.016
56592910 76057 None 1 Rat Functional pEC50 = 6.7 6.7 5 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2017.10.016
CHEMBL2057392 76057 None 1 Rat Functional pEC50 = 6.7 6.7 5 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2017.10.016
127044078 140375 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.10.016
CHEMBL3808485 140375 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.10.016
89777239 163953 None 24 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2017.10.016
CHEMBL4207737 163953 None 24 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2017.10.016
CHEMBL5268842 163953 None 24 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2017.10.016
135126266 164217 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)nc(Cl)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4210986 164217 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)nc(Cl)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
1505736 86292 None 11 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 337 2 2 4 4.2 Cc1nc2sc(C(=O)NC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313073 86292 None 11 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 337 2 2 4 4.2 Cc1nc2sc(C(=O)NC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
122191002 123612 None 0 Human Functional pEC50 = 6.6 6.6 -2 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccccc1F 10.1016/j.bmcl.2015.08.011
CHEMBL3618445 123612 None 0 Human Functional pEC50 = 6.6 6.6 -2 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccccc1F 10.1016/j.bmcl.2015.08.011
155551015 173970 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 379 4 0 6 3.1 COc1cccnc1C1CCN(C2CC3(CCN(c4cnccn4)C3)C2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4541697 173970 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 379 4 0 6 3.1 COc1cccnc1C1CCN(C2CC3(CCN(c4cnccn4)C3)C2)CC1 10.1021/acsmedchemlett.9b00106
3652 4097 None 79 Human Functional pEC50 = 6.6 6.6 -8 15
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
57 4097 None 79 Human Functional pEC50 = 6.6 6.6 -8 15
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
60809 4097 None 79 Human Functional pEC50 = 6.6 6.6 -8 15
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
60809.0 4097 None 79 Human Functional pEC50 = 6.6 6.6 -8 15
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
CHEMBL21536 4097 None 79 Human Functional pEC50 = 6.6 6.6 -8 15
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
DB15357 4097 None 79 Human Functional pEC50 = 6.6 6.6 -8 15
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
137650402 157163 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 453 4 2 6 2.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(S(N)(=O)=O)cc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4075391 157163 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 453 4 2 6 2.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(S(N)(=O)=O)cc2)CC1 10.1016/j.bmcl.2017.08.043
145963804 164072 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4209311 164072 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
145963804 164072 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4209311 164072 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
127043637 140529 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 381 3 0 6 4.3 Cc1sc2ncnc(N3CCC(Oc4ccc5c(c4)CCO5)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3810300 140529 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 381 3 0 6 4.3 Cc1sc2ncnc(N3CCC(Oc4ccc5c(c4)CCO5)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
155518790 170315 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 361 5 0 5 3.1 CCOC(=O)N1CCC(CN2CCC(c3ncccc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4446791 170315 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 361 5 0 5 3.1 CCOC(=O)N1CCC(CN2CCC(c3ncccc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
89777060 157121 None 0 Human Functional pEC50 = 7.6 7.6 114 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4074908 157121 None 0 Human Functional pEC50 = 7.6 7.6 114 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777113 149002 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942363 149002 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777113 149002 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942363 149002 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777226 159477 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 4 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(C(=O)OCc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4101598 159477 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 4 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(C(=O)OCc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89452445 173205 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 320 3 1 5 4.3 Cc1nc2sc3c(NCC4CC4)nn(C)c3c2c(C)c1Cl 10.1016/j.bmcl.2018.12.039
CHEMBL4522777 173205 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 320 3 1 5 4.3 Cc1nc2sc3c(NCC4CC4)nn(C)c3c2c(C)c1Cl 10.1016/j.bmcl.2018.12.039
137641641 158318 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 4 2 7 3.6 Cc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
CHEMBL4089170 158318 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 4 2 7 3.6 Cc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
162664650 182103 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 421 5 2 9 2.4 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4nnc(CC(C)C)o4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4781873 182103 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 421 5 2 9 2.4 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4nnc(CC(C)C)o4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
16371349 140456 None 6 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 459 5 2 7 2.5 Cc1sc2ncnc(N3CCC(C(=O)NCc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809384 140456 None 6 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 459 5 2 7 2.5 Cc1sc2ncnc(N3CCC(C(=O)NCc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
127043637 140529 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 381 3 0 6 4.3 Cc1sc2ncnc(N3CCC(Oc4ccc5c(c4)CCO5)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3810300 140529 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 381 3 0 6 4.3 Cc1sc2ncnc(N3CCC(Oc4ccc5c(c4)CCO5)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
137646437 157637 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4081305 157637 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5091043 215292 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc(C(C)(C)O)cc3F)ncnc12 10.1016/j.bmcl.2021.128416
CHEMBL5075610 214386 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(N3CCCC3)nccc12 10.1016/j.bmcl.2021.128416
CHEMBL5083833 214885 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(C3CCN(C(=O)C4(C)CC4)CC3)ncnc12 10.1016/j.bmcl.2021.128416
137658427 159724 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 467 5 2 8 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104561 159724 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 467 5 2 8 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
16371349 140456 None 6 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 459 5 2 7 2.5 Cc1sc2ncnc(N3CCC(C(=O)NCc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809384 140456 None 6 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 459 5 2 7 2.5 Cc1sc2ncnc(N3CCC(C(=O)NCc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
56592905 76056 None 1 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3cccnc3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057391 76056 None 1 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3cccnc3)nc12 10.1016/j.bmcl.2012.05.109
122189495 123335 None 0 Human Functional pEC50 = 6.6 6.6 -4 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 445 5 2 3 4.7 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616499 123335 None 0 Human Functional pEC50 = 6.6 6.6 -4 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 445 5 2 3 4.7 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
156016660 177707 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 5 2 6 4.1 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4642156 177707 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 5 2 6 4.1 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
155563393 175323 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4573723 175323 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
89777356 155882 None 0 Human Functional pEC50 = 7.6 7.6 72 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 3 2 6 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4060475 155882 None 0 Human Functional pEC50 = 7.6 7.6 72 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 3 2 6 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
155563393 175323 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4573723 175323 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
134207710 171422 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2nccn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4462813 171422 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2nccn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
156012527 177302 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 2 6 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4636668 177302 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 2 6 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
156014224 177257 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.3 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4636061 177257 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.3 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
156011921 177399 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 6 2.3 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4638291 177399 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 6 2.3 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
137650402 157163 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 453 4 2 6 2.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(S(N)(=O)=O)cc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4075391 157163 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 453 4 2 6 2.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(S(N)(=O)=O)cc2)CC1 10.1016/j.bmcl.2017.08.043
53382492 86333 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 352 3 2 6 3.5 Cc1nc2sc(C(=O)NCc3nccs3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313397 86333 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 352 3 2 6 3.5 Cc1nc2sc(C(=O)NCc3nccs3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89777356 155882 None 0 Human Functional pEC50 = 7.6 7.6 72 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 3 2 6 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4060475 155882 None 0 Human Functional pEC50 = 7.6 7.6 72 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 3 2 6 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
135153922 164656 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 364 5 1 7 2.4 COc1ccc(OC2CCN(c3nc(CO)nc(Cl)c3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4216650 164656 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 364 5 1 7 2.4 COc1ccc(OC2CCN(c3nc(CO)nc(Cl)c3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
155524827 170917 None 0 Human Functional pEC50 = 7.6 7.6 12 2
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 4 0 6 3.1 COc1cccnc1C1CCN(C2CCCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4455058 170917 None 0 Human Functional pEC50 = 7.6 7.6 12 2
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 4 0 6 3.1 COc1cccnc1C1CCN(C2CCCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
134207724 171765 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 495 3 2 8 3.8 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cc(C(F)(F)F)ncc5Cl)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4467568 171765 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 495 3 2 8 3.8 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cc(C(F)(F)F)ncc5Cl)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
89768534 151634 None 0 Human Functional pEC50 = 6.6 6.6 -14 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3963788 151634 None 0 Human Functional pEC50 = 6.6 6.6 -14 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
16071018 16054 None 20 Human Functional pEC50 = 6.6 6.6 -56 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16054 None 20 Human Functional pEC50 = 6.6 6.6 -56 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
155546031 173527 None 0 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
CHEMBL4531229 173527 None 0 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
89768534 151634 None 0 Human Functional pEC50 = 6.6 6.6 -14 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3963788 151634 None 0 Human Functional pEC50 = 6.6 6.6 -14 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
53382492 86333 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 352 3 2 6 3.5 Cc1nc2sc(C(=O)NCc3nccs3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313397 86333 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 352 3 2 6 3.5 Cc1nc2sc(C(=O)NCc3nccs3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
155532238 171706 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 403 5 0 8 3.2 COc1cccnc1C1CCN(C2CCCN(c3nsnc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4466730 171706 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 403 5 0 8 3.2 COc1cccnc1C1CCN(C2CCCN(c3nsnc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
44422692 11853 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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 11853 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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 11853 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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
44422699 11851 None 0 Human Functional pEC50 = 4.6 4.6 1 2
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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 11851 None 0 Human Functional pEC50 = 4.6 4.6 1 2
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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 11851 None 0 Human Functional pEC50 = 4.6 4.6 1 2
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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
155546031 173527 None 0 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
CHEMBL4531229 173527 None 0 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
156020148 178058 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 425 3 1 5 3.5 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(F)c(F)c2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4647297 178058 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 425 3 1 5 3.5 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(F)c(F)c2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL5085198 214956 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc4c(n3)CCC4)ncnc12 10.1016/j.bmcl.2021.128416
134207711 171161 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 3 2 7 2.7 Cc1cc2nncn2c2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4458791 171161 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 3 2 7 2.7 Cc1cc2nncn2c2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c12 10.1016/j.bmcl.2019.06.032
89777258 156765 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4070692 156765 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
75203027 170348 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 445 4 3 6 2.7 Cc1c[nH]c(=O)c2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4447294 170348 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 445 4 3 6 2.7 Cc1c[nH]c(=O)c2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL5088044 215134 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)oc1c(NC3CC3)ncnc12 10.1016/j.bmcl.2021.128416
89777269 158061 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 417 4 2 7 1.7 Cc1nnc2sc(C(=O)NC3CN(S(=O)(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4086111 158061 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 417 4 2 7 1.7 Cc1nnc2sc(C(=O)NC3CN(S(=O)(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777269 158061 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 417 4 2 7 1.7 Cc1nnc2sc(C(=O)NC3CN(S(=O)(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4086111 158061 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 417 4 2 7 1.7 Cc1nnc2sc(C(=O)NC3CN(S(=O)(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
53382484 86324 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccncn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313388 86324 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccncn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137645473 157596 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4080834 157596 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
134207712 173620 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 462 3 2 9 2.6 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5ncc(C(F)(F)F)cn5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4533701 173620 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 462 3 2 9 2.6 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5ncc(C(F)(F)F)cn5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207731 175216 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 2 2 5 3.3 Cc1cc2nccn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4571349 175216 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 2 2 5 3.3 Cc1cc2nccn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
41528344 170286 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 340 4 1 4 4.2 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2C)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4446337 170286 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 340 4 1 4 4.2 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2C)cc1 10.1016/j.bmcl.2018.12.039
117916916 174412 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 402 5 1 5 3.8 CCc1c(C(=O)NCc2ccc(S(C)(=O)=O)cc2)sc2nc(C)cc(C)c12 10.1016/j.bmcl.2018.12.039
CHEMBL4552714 174412 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 402 5 1 5 3.8 CCc1c(C(=O)NCc2ccc(S(C)(=O)=O)cc2)sc2nc(C)cc(C)c12 10.1016/j.bmcl.2018.12.039
53382484 86324 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccncn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313388 86324 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccncn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
44251554 7061 None 0 Rat Functional pEC50 = 5.6 5.6 -1 4
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M4. (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
CHEMBL1084941 7061 None 0 Rat Functional pEC50 = 5.6 5.6 -1 4
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M4. (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
156016190 177699 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 413 3 1 7 3.8 Cc1c2c(ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4642055 177699 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 413 3 1 7 3.8 Cc1c2c(ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL5086238 215016 None 2 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(N3CCCC3)ncnc12 10.1016/j.bmcl.2021.128416
137645473 157596 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4080834 157596 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137656219 159041 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4096833 159041 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
132063677 159233 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4098874 159233 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
24865895 96005 None 0 Human Functional pEC50 = 5.6 5.6 -6 2
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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 96005 None 0 Human Functional pEC50 = 5.6 5.6 -6 2
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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 96005 None 0 Human Functional pEC50 = 5.6 5.6 -6 2
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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
17413870 76061 None 7 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 285 3 1 5 3.0 COc1cccc2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057416 76061 None 7 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 285 3 1 5 3.0 COc1cccc2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2012.05.109
132063677 159233 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4098874 159233 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 6 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL5075538 214383 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(C)ncnc12 10.1016/j.bmcl.2021.128416
53382526 86306 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 339 2 2 5 3.1 Cc1nc2sc(C(=O)NC3CCOCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313370 86306 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 339 2 2 5 3.1 Cc1nc2sc(C(=O)NC3CCOCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382526 86306 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 339 2 2 5 3.1 Cc1nc2sc(C(=O)NC3CCOCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313370 86306 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 339 2 2 5 3.1 Cc1nc2sc(C(=O)NC3CCOCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
71719475 87587 None 0 Human Functional pEC50 = 7.5 7.5 -2 2
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 397 4 0 4 3.1 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@H](N3C(=O)Cc4ccccc43)C1)C2 10.1021/ml300372f
CHEMBL2336059 87587 None 0 Human Functional pEC50 = 7.5 7.5 -2 2
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 397 4 0 4 3.1 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@H](N3C(=O)Cc4ccccc43)C1)C2 10.1021/ml300372f
137658662 159430 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4101054 159430 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
2551 794 None 23 Human Functional pEC50 = 6.5 6.5 -4 13
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
2551.0 794 None 23 Human Functional pEC50 = 6.5 6.5 -4 13
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
298 794 None 23 Human Functional pEC50 = 6.5 6.5 -4 13
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
488 794 None 23 Human Functional pEC50 = 6.5 6.5 -4 13
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
CHEMBL965 794 None 23 Human Functional pEC50 = 6.5 6.5 -4 13
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
DB00411 794 None 23 Human Functional pEC50 = 6.5 6.5 -4 13
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
89768736 144289 None 0 Human Functional pEC50 = 6.5 6.5 -11 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 144289 None 0 Human Functional pEC50 = 6.5 6.5 -11 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
162651426 180198 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 340 2 3 6 2.2 Cc1c(O)nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4749546 180198 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 340 2 3 6 2.2 Cc1c(O)nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL5071551 214260 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc(S(C)(=O)=O)cc3)ncnc12 10.1016/j.bmcl.2021.128416
53382497 86323 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3cnccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313387 86323 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3cnccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
155543990 173321 None 0 Human Functional pEC50 = 6.5 6.5 4 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 402 5 1 7 4.0 Nc1c(C(=O)c2ccncc2)sc2nc(OCc3ccncc3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4526419 173321 None 0 Human Functional pEC50 = 6.5 6.5 4 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 402 5 1 7 4.0 Nc1c(C(=O)c2ccncc2)sc2nc(OCc3ccncc3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
89777257 159740 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4104862 159740 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
53382497 86323 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3cnccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313387 86323 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3cnccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137640924 157083 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 0 5 4.2 Cc1ccc2ncc(C#N)c(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2017.08.043
CHEMBL4074322 157083 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 0 5 4.2 Cc1ccc2ncc(C#N)c(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2017.08.043
155538474 173254 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 5 0 6 3.0 COc1cccnc1C1CCN(CC2CCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4524686 173254 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 5 0 6 3.0 COc1cccnc1C1CCN(CC2CCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
155561780 175766 None 0 Human Functional pEC50 = 8.5 8.5 1698 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 406 4 0 5 3.5 CCOC(=O)N1CCC2(CC(N3C[C@@H]4[C@H](c5nccn5-c5ccccc5)[C@@H]4C3)C2)C1 10.1021/acsmedchemlett.9b00106
CHEMBL4583597 175766 None 0 Human Functional pEC50 = 8.5 8.5 1698 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 406 4 0 5 3.5 CCOC(=O)N1CCC2(CC(N3C[C@@H]4[C@H](c5nccn5-c5ccccc5)[C@@H]4C3)C2)C1 10.1021/acsmedchemlett.9b00106
137656219 159041 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4096833 159041 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777226 159477 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 4 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(C(=O)OCc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4101598 159477 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 4 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(C(=O)OCc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
162673538 183050 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 442 3 2 7 3.6 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4794104 183050 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 442 3 2 7 3.6 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
89768546 149017 None 0 Rat Functional pEC50 = 7.5 7.5 18 3
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942511 149017 None 0 Rat Functional pEC50 = 7.5 7.5 18 3
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
44208359 16705 None 0 Human Functional pEC50 = 6.5 6.5 -23 3
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
CHEMBL1242979 16705 None 0 Human Functional pEC50 = 6.5 6.5 -23 3
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
16757565 15280 None 0 Rat Functional pEC50 = 6.5 6.5 -1 2
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1038/nchembio.2007.55
CHEMBL1212989 15280 None 0 Rat Functional pEC50 = 6.5 6.5 -1 2
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1038/nchembio.2007.55
CHEMBL2435356 15280 None 0 Rat Functional pEC50 = 6.5 6.5 -1 2
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1038/nchembio.2007.55
134207684 174578 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.0 Cc1cn2c(cc(C)c3c(N)c(C(=O)NC4Cc5cccnc5C4)sc32)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4556741 174578 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.0 Cc1cn2c(cc(C)c3c(N)c(C(=O)NC4Cc5cccnc5C4)sc32)n1 10.1016/j.bmcl.2019.06.032
53382530 86321 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313385 86321 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137640924 157083 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 0 5 4.2 Cc1ccc2ncc(C#N)c(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2017.08.043
CHEMBL4074322 157083 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 358 3 0 5 4.2 Cc1ccc2ncc(C#N)c(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2017.08.043
53382515 86307 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 1 2 4 3.7 Cc1nc2sc(C(=O)NC(C)(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313371 86307 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 1 2 4 3.7 Cc1nc2sc(C(=O)NC(C)(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
135125815 164513 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214738 164513 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
156010562 177046 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
156010562 177046 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4632555 177046 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632555 177046 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126812
53382515 86307 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 1 2 4 3.7 Cc1nc2sc(C(=O)NC(C)(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313371 86307 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 1 2 4 3.7 Cc1nc2sc(C(=O)NC(C)(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
135125815 164513 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214738 164513 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
42599070 16078 None 0 Human Functional pEC50 = 7.5 7.5 -79 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16078 None 0 Human Functional pEC50 = 7.5 7.5 -79 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
134207727 174983 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 4 2 6 3.4 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nccn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
CHEMBL4566449 174983 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 4 2 6 3.4 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nccn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
89777449 164017 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 336 4 1 5 3.2 CCCCC1(F)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4208486 164017 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 336 4 1 5 3.2 CCCCC1(F)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
89777449 164017 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 336 4 1 5 3.2 CCCCC1(F)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4208486 164017 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 336 4 1 5 3.2 CCCCC1(F)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
137634025 156634 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 347 3 0 4 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4069218 156634 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 347 3 0 4 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
89777257 159740 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4104862 159740 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccccc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137649175 157434 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4078814 157434 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
71528088 87586 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 387 4 1 5 1.6 CCOC(=O)N1CCC(O)(CN2CC[C@H](N3C(=O)Cc4ccccc43)C2)CC1 10.1021/ml300372f
CHEMBL2336057 87586 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 387 4 1 5 1.6 CCOC(=O)N1CCC(O)(CN2CC[C@H](N3C(=O)Cc4ccccc43)C2)CC1 10.1021/ml300372f
53382502 86326 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccnnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313390 86326 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccnnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145976573 163676 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 2 1 7 2.6 Cc1nnc2sc(C(=O)N3CC4(CCN(c5cccnc5)C4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4204671 163676 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 2 1 7 2.6 Cc1nnc2sc(C(=O)N3CC4(CCN(c5cccnc5)C4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
137658427 159724 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 467 5 2 8 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104561 159724 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 467 5 2 8 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137634025 156634 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 347 3 0 4 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4069218 156634 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 347 3 0 4 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
53382502 86326 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccnnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313390 86326 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ccnnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL5076867 214465 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc(C(C)(C)O)cc3)nccc12 10.1016/j.bmcl.2021.128416
89777179 156850 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4071560 156850 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137650247 157311 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4ccncn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4077183 157311 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4ccncn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
155554015 175690 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4581976 175690 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
145976835 163704 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
CHEMBL4204950 163704 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
155554015 175690 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4581976 175690 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
145976835 163704 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
CHEMBL4204950 163704 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 6 3.1 COc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
135125818 163964 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 4 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(F)c4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4207861 163964 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 4 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(F)c4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
135125818 163964 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 4 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(F)c4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4207861 163964 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 3 1 4 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(F)c4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
89777179 156850 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4071560 156850 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL5075035 214356 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NC3CC(c4ccncc4)C3)ncnc12 10.1016/j.bmcl.2021.128416
CHEMBL5085187 214954 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(-c3nccs3)ncnc12 10.1016/j.bmcl.2021.128416
155520521 170517 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3nccnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4449608 170517 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3nccnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
885513 173283 None 8 Human Functional pEC50 = 6.5 6.5 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4525501 173283 None 8 Human Functional pEC50 = 6.5 6.5 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
89777238 157027 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 3 2 8 2.7 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5o4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4073549 157027 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 3 2 8 2.7 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5o4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
53382540 86318 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313382 86318 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156013434 177507 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 6 1.6 Cc1c2c(N)c(C(=O)NC3CN(c4ncccc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4639628 177507 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 6 1.6 Cc1c2c(N)c(C(=O)NC3CN(c4ncccc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
155560153 174951 None 0 Rat Functional pEC50 = 5.5 5.5 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4565738 174951 None 0 Rat Functional pEC50 = 5.5 5.5 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
122191001 123611 None 0 Human Functional pEC50 = 6.5 6.5 -7 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1cccc(F)c1 10.1016/j.bmcl.2015.08.011
CHEMBL3618444 123611 None 0 Human Functional pEC50 = 6.5 6.5 -7 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1cccc(F)c1 10.1016/j.bmcl.2015.08.011
885513 173283 None 8 Human Functional pEC50 = 6.5 6.5 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4525501 173283 None 8 Human Functional pEC50 = 6.5 6.5 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
155520521 170517 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3nccnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4449608 170517 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3nccnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
155560153 174951 None 0 Rat Functional pEC50 = 5.5 5.5 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4565738 174951 None 0 Rat Functional pEC50 = 5.5 5.5 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
53382540 86318 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313382 86318 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL5089635 215219 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NC3CCC3)ncnc12 10.1016/j.bmcl.2021.128416
89777258 156765 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4070692 156765 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
156020077 178145 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4648817 178145 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
89777192 164409 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 294 1 1 5 2.1 Cc1nnc2sc(C(=O)N3CC(C)(F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4213420 164409 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 294 1 1 5 2.1 Cc1nnc2sc(C(=O)N3CC(C)(F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89777261 152900 None 0 Human Functional pEC50 = 6.4 6.4 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3974708 152900 None 0 Human Functional pEC50 = 6.4 6.4 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777192 164409 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 294 1 1 5 2.1 Cc1nnc2sc(C(=O)N3CC(C)(F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4213420 164409 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 294 1 1 5 2.1 Cc1nnc2sc(C(=O)N3CC(C)(F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89777261 152900 None 0 Human Functional pEC50 = 6.4 6.4 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3974708 152900 None 0 Human Functional pEC50 = 6.4 6.4 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
156013280 177491 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4639387 177491 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)c(N)c21 10.1016/j.bmcl.2019.126811
155540233 172905 None 0 Human Functional pEC50 = 7.4 7.4 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4516136 172905 None 0 Human Functional pEC50 = 7.4 7.4 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
155522645 170777 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2ncnn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4452874 170777 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2ncnn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
137649175 157434 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4078814 157434 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(F)cc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
156014638 177225 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.6 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ncc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4635575 177225 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.6 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ncc2nn1C 10.1016/j.bmcl.2019.126812
672747 172904 None 13 Human Functional pEC50 = 6.4 6.4 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4516088 172904 None 13 Human Functional pEC50 = 6.4 6.4 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
672747 172904 None 13 Human Functional pEC50 = 6.4 6.4 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4516088 172904 None 13 Human Functional pEC50 = 6.4 6.4 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
122191005 123614 None 0 Human Functional pEC50 = 5.4 5.4 -23 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 5 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618447 123614 None 0 Human Functional pEC50 = 5.4 5.4 -23 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 5 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
156018661 177835 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 387 4 2 8 1.2 COc1cc(N2CC(NC(=O)c3ccc4nnn(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4644004 177835 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 387 4 2 8 1.2 COc1cc(N2CC(NC(=O)c3ccc4nnn(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
156020827 178069 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.6 Cc1nn(C)c2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc12 10.1016/j.bmcl.2019.126812
CHEMBL4647393 178069 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.6 Cc1nn(C)c2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc12 10.1016/j.bmcl.2019.126812
156013839 177174 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 409 4 1 8 3.2 COc1cc(N2CC(Nc3ncnc4c3ccc3nn(C)c(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4634770 177174 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 409 4 1 8 3.2 COc1cc(N2CC(Nc3ncnc4c3ccc3nn(C)c(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
137650247 157311 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4ccncn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4077183 157311 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4ccncn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137640000 156737 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cncnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4070423 156737 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cncnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
155546031 173527 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
CHEMBL4531229 173527 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
885513 173283 None 8 Rat Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4525501 173283 None 8 Rat Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
155554015 175690 None 0 Rat Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4581976 175690 None 0 Rat Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155546031 173527 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
CHEMBL4531229 173527 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 359 5 1 6 3.9 COc1ccc(CCC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2016.07.042
885513 173283 None 8 Rat Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4525501 173283 None 8 Rat Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 298 2 2 5 3.4 Cc1cc(C)c2c(N)c(C(=O)c3ccc(O)cc3)sc2n1 10.1016/j.bmcl.2016.07.042
155554015 175690 None 0 Rat Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4581976 175690 None 0 Rat Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 319 2 1 5 3.4 Cc1nnc2sc(C(=O)c3ccc(F)cc3F)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
135126273 163882 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 5 3.5 COc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2017.10.016
CHEMBL4206946 163882 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 5 3.5 COc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2017.10.016
155546304 173540 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 300 3 2 4 4.4 Cc1cc(C)c2c(n1)sc1c(NCC3CCCC3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4531650 173540 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 300 3 2 4 4.4 Cc1cc(C)c2c(n1)sc1c(NCC3CCCC3)n[nH]c12 10.1016/j.bmcl.2018.12.039
24979170 21369 None 5 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 434 3 1 5 5.5 Cc1sc2ncnc(N3CCC(C(=O)Nc4cc(Cl)ccc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1314270 21369 None 5 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 434 3 1 5 5.5 Cc1sc2ncnc(N3CCC(C(=O)Nc4cc(Cl)ccc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
24979170 21369 None 5 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 434 3 1 5 5.5 Cc1sc2ncnc(N3CCC(C(=O)Nc4cc(Cl)ccc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1314270 21369 None 5 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 434 3 1 5 5.5 Cc1sc2ncnc(N3CCC(C(=O)Nc4cc(Cl)ccc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
135126273 163882 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 5 3.5 COc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2017.10.016
CHEMBL4206946 163882 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 5 3.5 COc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2017.10.016
156009502 177102 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4c(C)n(C)nc4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4633344 177102 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4c(C)n(C)nc4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
30270932 140413 None 8 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 4 2 6 3.3 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(C(N)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808920 140413 None 8 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 4 2 6 3.3 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(C(N)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
135126256 164571 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4215358 164571 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
42598591 16077 None 0 Human Functional pEC50 = 7.4 7.4 -79 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16077 None 0 Human Functional pEC50 = 7.4 7.4 -79 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
30270932 140413 None 8 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 4 2 6 3.3 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(C(N)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808920 140413 None 8 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 4 2 6 3.3 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(C(N)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
11081520 118973 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity against human M4 muscarinic receptor expressed in RBL-2H3 Mast cellsAgonist activity against human M4 muscarinic receptor expressed in RBL-2H3 Mast cells
ChEMBL 420 7 0 10 2.3 CN1CCC=C(c2nsnc2OCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL342400 118973 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity against human M4 muscarinic receptor expressed in RBL-2H3 Mast cellsAgonist activity against human M4 muscarinic receptor expressed in RBL-2H3 Mast cells
ChEMBL 420 7 0 10 2.3 CN1CCC=C(c2nsnc2OCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL5094699 215512 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(C3CC3)ncnc12 10.1016/j.bmcl.2021.128416
135126256 164571 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4215358 164571 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
122191007 123616 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 449 5 2 3 4.5 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618449 123616 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 449 5 2 3 4.5 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
122189496 123336 None 0 Human Functional pEC50 = 6.4 6.4 -10 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 499 5 2 3 5.4 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C(F)(F)F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616500 123336 None 0 Human Functional pEC50 = 6.4 6.4 -10 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 499 5 2 3 5.4 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C(F)(F)F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
145964223 164456 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214008 164456 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
19571628 175381 None 0 Rat Functional pEC50 = 5.4 5.4 -7 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4575082 175381 None 0 Rat Functional pEC50 = 5.4 5.4 -7 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
2551 794 None 23 Human Functional pEC50 = 5.4 5.4 -4 13
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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
2551.0 794 None 23 Human Functional pEC50 = 5.4 5.4 -4 13
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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
298 794 None 23 Human Functional pEC50 = 5.4 5.4 -4 13
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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
488 794 None 23 Human Functional pEC50 = 5.4 5.4 -4 13
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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 794 None 23 Human Functional pEC50 = 5.4 5.4 -4 13
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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 794 None 23 Human Functional pEC50 = 5.4 5.4 -4 13
Agonist activity at human muscarinic M4 receptor expressed in CHO cellsAgonist activity at human muscarinic M4 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
19571628 175381 None 0 Rat Functional pEC50 = 5.4 5.4 -7 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4575082 175381 None 0 Rat Functional pEC50 = 5.4 5.4 -7 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
10952416 35150 None 0 Human Functional pEC50 = 8.3 8.3 323 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 578 16 0 10 7.2 CN1CCC=C(c2nsnc2SCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143466 35150 None 0 Human Functional pEC50 = 8.3 8.3 323 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 578 16 0 10 7.2 CN1CCC=C(c2nsnc2SCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
87057216 172250 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 4 1 7 3.8 COc1ccc(CNc2nn(C)c3c2sc2nnc(C)c(C)c23)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4474325 172250 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 4 1 7 3.8 COc1ccc(CNc2nn(C)c3c2sc2nnc(C)c(C)c23)cc1 10.1016/j.bmcl.2018.12.039
135409468 2035 None 69 Human Functional pEC50 = 6.4 6.4 -7 5
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 2035 None 69 Human Functional pEC50 = 6.4 6.4 -7 5
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 2035 None 69 Human Functional pEC50 = 6.4 6.4 -7 5
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
154733029 4017 None 59 Rat Functional pEC50 = 6.4 6.4 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 10.1038/nchembio.2007.55
7633 4017 None 59 Rat Functional pEC50 = 6.4 6.4 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 10.1038/nchembio.2007.55
CHEMBL1212994 4017 None 59 Rat Functional pEC50 = 6.4 6.4 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 10.1038/nchembio.2007.55
145964223 164456 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214008 164456 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL5085688 214981 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc(OC(F)F)cc3)ncnc12 10.1016/j.bmcl.2021.128416
122191008 123617 None 0 Human Functional pEC50 = 6.4 6.4 -13 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 465 5 2 3 5.0 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Cl)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618450 123617 None 0 Human Functional pEC50 = 6.4 6.4 -13 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 465 5 2 3 5.0 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Cl)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
145973064 164654 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216633 164654 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145976573 163676 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 2 1 7 2.6 Cc1nnc2sc(C(=O)N3CC4(CCN(c5cccnc5)C4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4204671 163676 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 2 1 7 2.6 Cc1nnc2sc(C(=O)N3CC4(CCN(c5cccnc5)C4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145973064 164654 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216633 164654 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccccc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
137640000 156737 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cncnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4070423 156737 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cncnc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
134207729 174184 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 424 4 2 10 2.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5nnc(C6CC6)o5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4547561 174184 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 424 4 2 10 2.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5nnc(C6CC6)o5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
16309462 26188 None 4 Human Functional pEC50 = 6.4 6.4 -4 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1357034 26188 None 4 Human Functional pEC50 = 6.4 6.4 -4 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
155539719 172873 None 0 Rat Functional pEC50 = 6.4 6.4 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4515326 172873 None 0 Rat Functional pEC50 = 6.4 6.4 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155564640 175515 None 0 Rat Functional pEC50 = 6.4 6.4 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4577985 175515 None 0 Rat Functional pEC50 = 6.4 6.4 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
89777032 163760 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 3 1 6 3.0 COC1(c2cccc(F)c2)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4205587 163760 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 3 1 6 3.0 COC1(c2cccc(F)c2)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
53382513 86308 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 327 5 2 5 2.9 COCCCNC(=O)c1sc2nc(C)c(Cl)c(C)c2c1N 10.1016/j.bmcl.2012.10.073
CHEMBL2313372 86308 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 327 5 2 5 2.9 COCCCNC(=O)c1sc2nc(C)c(Cl)c(C)c2c1N 10.1016/j.bmcl.2012.10.073
89777190 143035 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3cccc(S(C)(=O)=O)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3894866 143035 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3cccc(S(C)(=O)=O)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
155539719 172873 None 0 Rat Functional pEC50 = 6.4 6.4 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4515326 172873 None 0 Rat Functional pEC50 = 6.4 6.4 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155553146 174077 None 0 Rat Functional pEC50 = 6.4 6.4 -5 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 424 6 1 8 2.7 Nc1c(C(=O)c2ccncc2)sc2nc(OCCN3CCOCC3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4544318 174077 None 0 Rat Functional pEC50 = 6.4 6.4 -5 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 424 6 1 8 2.7 Nc1c(C(=O)c2ccncc2)sc2nc(OCCN3CCOCC3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
155564640 175515 None 0 Rat Functional pEC50 = 6.4 6.4 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4577985 175515 None 0 Rat Functional pEC50 = 6.4 6.4 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
89777032 163760 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 3 1 6 3.0 COC1(c2cccc(F)c2)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4205587 163760 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 3 1 6 3.0 COC1(c2cccc(F)c2)CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
89777190 143035 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3cccc(S(C)(=O)=O)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3894866 143035 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3cccc(S(C)(=O)=O)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
53382513 86308 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 327 5 2 5 2.9 COCCCNC(=O)c1sc2nc(C)c(Cl)c(C)c2c1N 10.1016/j.bmcl.2012.10.073
CHEMBL2313372 86308 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 327 5 2 5 2.9 COCCCNC(=O)c1sc2nc(C)c(Cl)c(C)c2c1N 10.1016/j.bmcl.2012.10.073
89777238 157027 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 3 2 8 2.7 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5o4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4073549 157027 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 394 3 2 8 2.7 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5o4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
156010493 177083 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4633152 177083 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1c2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2nn1C 10.1016/j.bmcl.2019.126812
127044525 140520 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 374 3 0 6 4.4 Cc1sc2ncnc(N3CCC(Oc4ccc(Cl)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3810183 140520 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 374 3 0 6 4.4 Cc1sc2ncnc(N3CCC(Oc4ccc(Cl)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
187 255 None 39 Human Functional pEC50 = 7.4 7.4 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
187.0 255 None 39 Human Functional pEC50 = 7.4 7.4 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
294 255 None 39 Human Functional pEC50 = 7.4 7.4 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
65 255 None 39 Human Functional pEC50 = 7.4 7.4 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
8593 255 None 39 Human Functional pEC50 = 7.4 7.4 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
CHEMBL667 255 None 39 Human Functional pEC50 = 7.4 7.4 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
DB03128 255 None 39 Human Functional pEC50 = 7.4 7.4 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
156014184 177197 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cn4c(C)c(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4635170 177197 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cn4c(C)c(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
127044525 140520 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 374 3 0 6 4.4 Cc1sc2ncnc(N3CCC(Oc4ccc(Cl)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3810183 140520 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 374 3 0 6 4.4 Cc1sc2ncnc(N3CCC(Oc4ccc(Cl)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
89768704 158441 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 2 8 3.1 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4090463 158441 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 2 8 3.1 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
145971419 164680 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4216930 164680 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
127043632 140372 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 355 3 0 7 3.5 Cc1ncc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3808442 140372 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 355 3 0 7 3.5 Cc1ncc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
89768704 158441 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 2 8 3.1 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4090463 158441 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 2 8 3.1 Cc1nnc2sc(C(=O)NC3CN(c4nc5ccccc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777222 150577 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 432 4 2 7 3.4 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3955059 150577 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 432 4 2 7 3.4 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777222 150577 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 432 4 2 7 3.4 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3955059 150577 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 432 4 2 7 3.4 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
145971419 164680 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4216930 164680 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
127043632 140372 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 355 3 0 7 3.5 Cc1ncc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3808442 140372 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 355 3 0 7 3.5 Cc1ncc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
89777270 163647 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 374 2 1 5 3.4 Cc1nnc2sc(C(=O)N3CC(F)(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4204144 163647 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 374 2 1 5 3.4 Cc1nnc2sc(C(=O)N3CC(F)(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145975083 163636 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203977 163636 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
89777270 163647 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 374 2 1 5 3.4 Cc1nnc2sc(C(=O)N3CC(F)(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4204144 163647 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 374 2 1 5 3.4 Cc1nnc2sc(C(=O)N3CC(F)(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145975083 163636 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203977 163636 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
156019934 177963 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 3 2 7 1.2 Cn1nnc2ccc(C(=O)NC3CN(c4cccc(Cl)n4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4645945 177963 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 357 3 2 7 1.2 Cn1nnc2ccc(C(=O)NC3CN(c4cccc(Cl)n4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL5082438 214802 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(N3CC4CC4C3)ncnc12 10.1016/j.bmcl.2021.128416
145965409 164056 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4209083 164056 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
156012624 177419 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)n(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4638506 177419 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)n(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL5073777 214306 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(N3CC(F)(F)C3)ncnc12 10.1016/j.bmcl.2021.128416
145968703 164796 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4218342 164796 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
145968703 164796 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
CHEMBL4218342 164796 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccccc1C1CN(C(=O)c2sc3nnc(C)c(C)c3c2N)C1 10.1016/j.bmcl.2017.10.053
145965409 164056 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4209083 164056 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 3 1 4 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
134207719 175889 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4Cc5ccccc5C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4586356 175889 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4Cc5ccccc5C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
156010345 177074 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 8 1.1 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4633013 177074 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 8 1.1 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
156022245 177222 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 268 1 0 4 3.4 Cc1c2c(ccc3c(CC(C)(C)C)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4635539 177222 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 268 1 0 4 3.4 Cc1c2c(ccc3c(CC(C)(C)C)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
156011257 177328 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 443 3 1 5 3.9 Cn1c(C(F)(F)F)nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
CHEMBL4637175 177328 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 443 3 1 5 3.9 Cn1c(C(F)(F)F)nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
72945087 120541 None 1 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at muscarinic M4 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M4 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
CHEMBL3310802 120541 None 1 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at muscarinic M4 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M4 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
CHEMBL3545481 120541 None 1 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at muscarinic M4 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M4 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
89777278 151917 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 418 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3966208 151917 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 418 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777278 151917 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 418 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3966208 151917 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 418 5 2 7 3.0 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(C)C)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
155523539 170889 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 387 4 0 7 3.5 COc1cccnc1C1CCN(C2CCCN(c3nsnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4454446 170889 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 387 4 0 7 3.5 COc1cccnc1C1CCN(C2CCCN(c3nsnc3C)CC2)CC1 10.1021/acsmedchemlett.9b00106
156014219 177247 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 351 4 1 6 3.6 COc1ccc(CNc2ncnc3c2ccc2nn(C)c(C)c23)cc1F 10.1016/j.bmcl.2019.126811
CHEMBL4635909 177247 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 351 4 1 6 3.6 COc1ccc(CNc2ncnc3c2ccc2nn(C)c(C)c23)cc1F 10.1016/j.bmcl.2019.126811
156012754 177311 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 5 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4636845 177311 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 5 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
155520162 173245 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4524555 173245 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
698706 175539 None 21 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4578455 175539 None 21 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
155520162 173245 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4524555 173245 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
698706 175539 None 21 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4578455 175539 None 21 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
187 255 None 39 Human Functional pEC50 = 7.3 7.3 1 8
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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
187.0 255 None 39 Human Functional pEC50 = 7.3 7.3 1 8
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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
294 255 None 39 Human Functional pEC50 = 7.3 7.3 1 8
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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
65 255 None 39 Human Functional pEC50 = 7.3 7.3 1 8
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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 255 None 39 Human Functional pEC50 = 7.3 7.3 1 8
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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 255 None 39 Human Functional pEC50 = 7.3 7.3 1 8
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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 255 None 39 Human Functional pEC50 = 7.3 7.3 1 8
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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
89777463 158811 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4094439 158811 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
698706 175539 None 21 Rat Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4578455 175539 None 21 Rat Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
137652430 157526 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 0 5 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(F)nc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4079953 157526 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 0 5 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(F)nc2)CC1 10.1016/j.bmcl.2017.08.043
698706 175539 None 21 Rat Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4578455 175539 None 21 Rat Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 312 3 1 5 3.7 COc1ccc(C(=O)c2sc3nc(C)cc(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
156019515 177980 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 392 3 1 5 3.9 Cc1nc2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2s1 10.1016/j.bmcl.2019.126812
CHEMBL4646040 177980 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 392 3 1 5 3.9 Cc1nc2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2s1 10.1016/j.bmcl.2019.126812
3263 4025 None 58 Human Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2021.128416
864492 4025 None 58 Human Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2021.128416
CHEMBL1978713 4025 None 58 Human Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2021.128416
9809330 115999 None 0 Human Functional pEC50 = 8.3 8.3 -8 3
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL335542 115999 None 0 Human Functional pEC50 = 8.3 8.3 -8 3
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
306 3456 None 21 Human Functional pEC50 = 8.2 8.2 1 5
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/ml300372f
3536 3456 None 21 Human Functional pEC50 = 8.2 8.2 1 5
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/ml300372f
53930639 3456 None 21 Human Functional pEC50 = 8.2 8.2 1 5
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/ml300372f
9577995 3456 None 21 Human Functional pEC50 = 8.2 8.2 1 5
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/ml300372f
CHEMBL134641 3456 None 21 Human Functional pEC50 = 8.2 8.2 1 5
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/ml300372f
137653452 158604 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)ccn1 10.1016/j.bmcl.2017.05.014
CHEMBL4092128 158604 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)ccn1 10.1016/j.bmcl.2017.05.014
45142486 52359 None 0 Human Functional pEC50 = 6.3 6.3 2 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1016/j.bmcl.2012.10.073
CHEMBL1589763 52359 None 0 Human Functional pEC50 = 6.3 6.3 2 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1016/j.bmcl.2012.10.073
42598829 16080 None 0 Human Functional pEC50 = 6.3 6.3 -63 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16080 None 0 Human Functional pEC50 = 6.3 6.3 -63 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
42599071 16124 None 0 Human Functional pEC50 = 6.3 6.3 -199 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16124 None 0 Human Functional pEC50 = 6.3 6.3 -199 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
16071018 16054 None 20 Human Functional pEC50 = 6.3 6.3 -56 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit 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 16054 None 20 Human Functional pEC50 = 6.3 6.3 -56 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit 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
137653452 158604 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)ccn1 10.1016/j.bmcl.2017.05.014
CHEMBL4092128 158604 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)ccn1 10.1016/j.bmcl.2017.05.014
89777261 152900 None 0 Rat Functional pEC50 = 7.3 7.3 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3974708 152900 None 0 Rat Functional pEC50 = 7.3 7.3 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777261 152900 None 0 Rat Functional pEC50 = 7.3 7.3 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3974708 152900 None 0 Rat Functional pEC50 = 7.3 7.3 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 390 4 2 7 2.2 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
162655852 180722 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 437 4 2 8 2.6 CCc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4755728 180722 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 437 4 2 8 2.6 CCc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
117916853 174198 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 326 4 1 4 3.9 COc1ccc(CNC(=O)c2cc3c(C)cc(C)nc3s2)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4547995 174198 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 326 4 1 4 3.9 COc1ccc(CNC(=O)c2cc3c(C)cc(C)nc3s2)cc1 10.1016/j.bmcl.2018.12.039
137652430 157526 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 0 5 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(F)nc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4079953 157526 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 0 5 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(F)nc2)CC1 10.1016/j.bmcl.2017.08.043
53382498 86336 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 325 2 2 5 2.7 Cc1nc2sc(C(=O)NC3CCOC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313402 86336 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 325 2 2 5 2.7 Cc1nc2sc(C(=O)NC3CCOC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382498 86336 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 325 2 2 5 2.7 Cc1nc2sc(C(=O)NC3CCOC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313402 86336 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 325 2 2 5 2.7 Cc1nc2sc(C(=O)NC3CCOC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156019814 177384 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 295 1 0 6 1.7 Cc1c2c(ccc3c(N4CC5(COC5)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4638044 177384 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 295 1 0 6 1.7 Cc1c2c(ccc3c(N4CC5(COC5)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
155520162 173245 None 0 Rat Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4524555 173245 None 0 Rat Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
137637726 155890 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)c(F)n1 10.1016/j.bmcl.2017.08.043
CHEMBL4060527 155890 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)c(F)n1 10.1016/j.bmcl.2017.08.043
11498 3019 None 41 Human Functional pEC50 = 7.3 7.3 13 5
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
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 3019 None 41 Human Functional pEC50 = 7.3 7.3 13 5
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
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 3019 None 41 Human Functional pEC50 = 7.3 7.3 13 5
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
137633999 156556 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4068328 156556 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
155520162 173245 None 0 Rat Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4524555 173245 None 0 Rat Functional pEC50 = 6.3 6.3 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 311 4 1 5 3.7 Cc1cc(C)c2c(N)c(C(=O)CCc3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
162667175 182401 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 451 4 2 8 3.1 Cc1c(C(C)C)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4785538 182401 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 451 4 2 8 3.1 Cc1c(C(C)C)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
89768546 149017 None 0 Human Functional pEC50 = 6.3 6.3 -18 3
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942511 149017 None 0 Human Functional pEC50 = 6.3 6.3 -18 3
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89768546 149017 None 0 Human Functional pEC50 = 6.3 6.3 -18 3
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942511 149017 None 0 Human Functional pEC50 = 6.3 6.3 -18 3
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
156013700 177275 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 361 4 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4636269 177275 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 361 4 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4640311 177275 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 361 4 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
137633999 156556 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4068328 156556 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
53382523 76062 None 0 Human Functional pEC50 = 7.3 7.3 3 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2057417 76062 None 0 Human Functional pEC50 = 7.3 7.3 3 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382523 76062 None 0 Human Functional pEC50 = 7.3 7.3 3 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2057417 76062 None 0 Human Functional pEC50 = 7.3 7.3 3 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
117917123 171691 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 5 1 5 4.3 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2C2CC2)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL4466551 171691 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 5 1 5 4.3 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2C2CC2)cc1F 10.1016/j.bmcl.2018.12.039
19571628 175381 None 0 Human Functional pEC50 = 6.3 6.3 7 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4575082 175381 None 0 Human Functional pEC50 = 6.3 6.3 7 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
19571628 175381 None 0 Human Functional pEC50 = 6.3 6.3 7 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4575082 175381 None 0 Human Functional pEC50 = 6.3 6.3 7 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 318 2 1 4 4.0 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)cc3F)sc2n1 10.1016/j.bmcl.2016.07.042
53002564 157142 None 6 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 1 4 4.4 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4075147 157142 None 6 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 1 4 4.4 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2017.08.043
89777274 158752 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4093866 158752 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137653326 158846 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4cc(F)c(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4094821 158846 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4cc(F)c(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
137657888 159689 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 0 5 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(Cl)nc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4104193 159689 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 0 5 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(Cl)nc2)CC1 10.1016/j.bmcl.2017.08.043
89777274 158752 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4093866 158752 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137637726 155890 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)c(F)n1 10.1016/j.bmcl.2017.08.043
CHEMBL4060527 155890 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)c(F)n1 10.1016/j.bmcl.2017.08.043
53002564 157142 None 6 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 1 4 4.4 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4075147 157142 None 6 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 410 3 1 4 4.4 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2017.08.043
145973726 164630 None 0 Human Functional pEC50 = 7.2 7.2 36 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216213 164630 None 0 Human Functional pEC50 = 7.2 7.2 36 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
187 255 None 39 Human Functional pEC50 = 7.2 7.2 1 8
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
187.0 255 None 39 Human Functional pEC50 = 7.2 7.2 1 8
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
294 255 None 39 Human Functional pEC50 = 7.2 7.2 1 8
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
65 255 None 39 Human Functional pEC50 = 7.2 7.2 1 8
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
8593 255 None 39 Human Functional pEC50 = 7.2 7.2 1 8
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
CHEMBL667 255 None 39 Human Functional pEC50 = 7.2 7.2 1 8
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
DB03128 255 None 39 Human Functional pEC50 = 7.2 7.2 1 8
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acsmedchemlett.9b00106
145973726 164630 None 0 Human Functional pEC50 = 7.2 7.2 36 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216213 164630 None 0 Human Functional pEC50 = 7.2 7.2 36 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89777153 143245 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 4 2 7 2.4 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3896591 143245 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 4 2 7 2.4 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777153 143245 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 4 2 7 2.4 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3896591 143245 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 4 2 7 2.4 Cc1nnc2sc(C(=O)NCc3ccc(S(C)(=O)=O)c(F)c3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
18204435 37445 None 5 Human Functional pEC50 = 6.2 6.2 48 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 423 4 2 6 3.5 CNC(=O)c1ccc(NC(=O)C2CCN(c3ncnc4sc(C)c(C)c34)CC2)cc1 10.1016/j.bmcl.2016.05.010
CHEMBL1455259 37445 None 5 Human Functional pEC50 = 6.2 6.2 48 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 423 4 2 6 3.5 CNC(=O)c1ccc(NC(=O)C2CCN(c3ncnc4sc(C)c(C)c34)CC2)cc1 10.1016/j.bmcl.2016.05.010
137653326 158846 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4cc(F)c(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4094821 158846 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4cc(F)c(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
18204435 37445 None 5 Human Functional pEC50 = 6.2 6.2 48 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 423 4 2 6 3.5 CNC(=O)c1ccc(NC(=O)C2CCN(c3ncnc4sc(C)c(C)c34)CC2)cc1 10.1016/j.bmcl.2016.05.010
CHEMBL1455259 37445 None 5 Human Functional pEC50 = 6.2 6.2 48 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 423 4 2 6 3.5 CNC(=O)c1ccc(NC(=O)C2CCN(c3ncnc4sc(C)c(C)c34)CC2)cc1 10.1016/j.bmcl.2016.05.010
127044078 140375 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3808485 140375 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
137657888 159689 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 0 5 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(Cl)nc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4104193 159689 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 0 5 4.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2ccc(Cl)nc2)CC1 10.1016/j.bmcl.2017.08.043
89777463 158811 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4094439 158811 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccnc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
71683155 157192 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 7 2.8 Cc1cccc(OC(=O)N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4075751 157192 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 7 2.8 Cc1cccc(OC(=O)N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
156016804 177722 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 403 4 1 5 3.5 CCc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4642310 177722 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 403 4 1 5 3.5 CCc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126812
145975343 163680 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4204738 163680 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
155544229 173372 None 0 Human Functional pEC50 = 6.2 6.2 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4527640 173372 None 0 Human Functional pEC50 = 6.2 6.2 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
45501063 157208 None 10 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccccc1CNC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4076022 157208 None 10 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccccc1CNC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
145975343 163680 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4204738 163680 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 4.2 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(Cl)cc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
155544229 173372 None 0 Human Functional pEC50 = 6.2 6.2 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4527640 173372 None 0 Human Functional pEC50 = 6.2 6.2 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1cc(C)c2c(N)c(C(=O)c3ccncc3)sc2n1 10.1016/j.bmcl.2016.07.042
117916866 174881 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 3 1 4 4.1 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc4c(c3)CCO4)sc2n1 10.1016/j.bmcl.2018.12.039
CHEMBL4563934 174881 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 3 1 4 4.1 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc4c(c3)CCO4)sc2n1 10.1016/j.bmcl.2018.12.039
156017788 177815 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 4 1 7 2.7 COc1ccc(CNc2ncnc3c2ccc2nnn(C)c23)cc1F 10.1016/j.bmcl.2019.126811
CHEMBL4643687 177815 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 4 1 7 2.7 COc1ccc(CNc2ncnc3c2ccc2nnn(C)c23)cc1F 10.1016/j.bmcl.2019.126811
3652 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
57 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
60809 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
60809.0 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
CHEMBL21536 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
DB15357 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
3652 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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
60809.0 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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 4097 None 79 Human Functional pEC50 = 8.2 8.2 -8 15
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit 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
86292822 171168 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 1 8 3.6 Cc1nnc2sc3c(NCc4ccc5c(c4)OCCO5)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4458844 171168 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 1 8 3.6 Cc1nnc2sc3c(NCc4ccc5c(c4)OCCO5)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
134207680 173581 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 2 2 7 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4Cc5cccnc5C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4532897 173581 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 2 2 7 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4Cc5cccnc5C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
162652818 180378 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 324 2 2 5 2.5 Cc1cnnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4751679 180378 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 324 2 2 5 2.5 Cc1cnnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
134265583 182008 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 443 3 2 8 2.7 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4780651 182008 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 443 3 2 8 2.7 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
89777143 153842 None 0 Human Functional pEC50 = 7.2 7.2 -5 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3982695 153842 None 0 Human Functional pEC50 = 7.2 7.2 -5 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
89777143 153842 None 0 Human Functional pEC50 = 7.2 7.2 -5 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3982695 153842 None 0 Human Functional pEC50 = 7.2 7.2 -5 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
127044078 140375 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3808485 140375 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
127043635 140429 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 354 3 0 6 4.1 Cc1ccc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3809096 140429 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 354 3 0 6 4.1 Cc1ccc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
53382520 86314 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313378 86314 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
973723 15278 None 12 Rat Functional pEC50 = 5.2 5.2 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 263 2 2 4 2.6 Cc1cc(C)c2c(N)c(C(=O)NC(C)C)sc2n1 10.1038/nchembio.2007.55
CHEMBL1212982 15278 None 12 Rat Functional pEC50 = 5.2 5.2 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 263 2 2 4 2.6 Cc1cc(C)c2c(N)c(C(=O)NC(C)C)sc2n1 10.1038/nchembio.2007.55
2551 794 None 23 Human Functional pEC50 = 4.2 4.2 -4 13
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
2551.0 794 None 23 Human Functional pEC50 = 4.2 4.2 -4 13
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 794 None 23 Human Functional pEC50 = 4.2 4.2 -4 13
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 794 None 23 Human Functional pEC50 = 4.2 4.2 -4 13
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 794 None 23 Human Functional pEC50 = 4.2 4.2 -4 13
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 794 None 23 Human Functional pEC50 = 4.2 4.2 -4 13
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
89777146 159677 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 2 6 2.1 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104033 159677 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 2 6 2.1 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
127043635 140429 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 354 3 0 6 4.1 Cc1ccc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3809096 140429 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 354 3 0 6 4.1 Cc1ccc(OC2CCN(c3ncnc4sc(C)c(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
53382520 86314 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313378 86314 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382524 86315 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 3.8 Cc1cc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)ccn1 10.1016/j.bmcl.2012.10.073
CHEMBL2313379 86315 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 3.8 Cc1cc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)ccn1 10.1016/j.bmcl.2012.10.073
53382524 86315 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 3.8 Cc1cc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)ccn1 10.1016/j.bmcl.2012.10.073
CHEMBL2313379 86315 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 3.8 Cc1cc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)ccn1 10.1016/j.bmcl.2012.10.073
CHEMBL5085621 214976 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(C3CCNCC3)ncnc12 10.1016/j.bmcl.2021.128416
135126264 164519 None 0 Rat Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 5 1 6 3.0 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(OC(C)C)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214822 164519 None 0 Rat Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 5 1 6 3.0 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(OC(C)C)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137633344 156305 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4065477 156305 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
45501064 156358 None 12 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1 10.1016/j.bmcl.2017.08.043
CHEMBL4065963 156358 None 12 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1 10.1016/j.bmcl.2017.08.043
55485382 140406 None 5 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 2 6 3.7 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(N5CCNC5=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808847 140406 None 5 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 2 6 3.7 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(N5CCNC5=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
135126264 164519 None 0 Rat Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 5 1 6 3.0 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(OC(C)C)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4214822 164519 None 0 Rat Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 5 1 6 3.0 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncc(OC(C)C)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137633344 156305 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4065477 156305 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
156017195 177696 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 5 2.4 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4642005 177696 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 371 3 2 5 2.4 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
87057214 176147 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 287 3 1 6 3.0 Cc1nnc2sc3c(NCC4CC4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4592523 176147 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 287 3 1 6 3.0 Cc1nnc2sc3c(NCC4CC4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
134207689 176132 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 440 3 2 10 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5nnc(C(C)(C)C)o5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4592120 176132 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 440 3 2 10 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5nnc(C(C)(C)C)o5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
3263 4025 None 58 Human Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
864492 4025 None 58 Human Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
CHEMBL1978713 4025 None 58 Human Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
CHEMBL5089728 215224 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(C3CCN(C(=O)C4CC4)CC3)ncnc12 10.1016/j.bmcl.2021.128416
55485382 140406 None 5 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 2 6 3.7 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(N5CCNC5=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808847 140406 None 5 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 2 6 3.7 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(N5CCNC5=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
156012048 177403 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 7 1.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(F)cn4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4638318 177403 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 7 1.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(F)cn4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
156010237 177041 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 267 1 0 5 2.4 Cc1c2c(ccc3c(N4CCCC4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632514 177041 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 267 1 0 5 2.4 Cc1c2c(ccc3c(N4CCCC4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
156015762 177544 None 0 Human Functional pEC50 = 7.2 7.2 2 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 8 2.9 Cn1nnc2ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL4640254 177544 None 0 Human Functional pEC50 = 7.2 7.2 2 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 8 2.9 Cn1nnc2ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc3c21 10.1016/j.bmcl.2019.126811
89777104 159123 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4097819 159123 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
89777437 159512 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccc(F)nc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4102040 159512 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccc(F)nc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
16123945 80459 None 12 Human Functional pEC50 = 6.2 6.2 -125 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit 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 80459 None 12 Human Functional pEC50 = 6.2 6.2 -125 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit 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
137647278 157923 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 3 0 5 4.1 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3c(C#N)cnc4ccc(F)cc34)CC1)C2 10.1016/j.bmcl.2017.08.043
CHEMBL4084404 157923 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 3 0 5 4.1 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3c(C#N)cnc4ccc(F)cc34)CC1)C2 10.1016/j.bmcl.2017.08.043
12301 4047 None 30 Human Functional pEC50 = 6.2 6.2 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
73774630 4047 None 30 Human Functional pEC50 = 6.2 6.2 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 4047 None 30 Human Functional pEC50 = 6.2 6.2 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
53002537 157065 None 1 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 2 0 5 2.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCOCC2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4074092 157065 None 1 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 2 0 5 2.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCOCC2)CC1 10.1016/j.bmcl.2017.08.043
12301 4047 None 30 Human Functional pEC50 = 6.2 6.2 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
73774630 4047 None 30 Human Functional pEC50 = 6.2 6.2 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 4047 None 30 Human Functional pEC50 = 6.2 6.2 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
89777437 159512 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccc(F)nc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4102040 159512 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccc(F)nc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
117916898 173314 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 5 3.6 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc(S(C)(=O)=O)cc3)sc2n1 10.1016/j.bmcl.2018.12.039
CHEMBL4526215 173314 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 5 3.6 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc(S(C)(=O)=O)cc3)sc2n1 10.1016/j.bmcl.2018.12.039
53002537 157065 None 1 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 2 0 5 2.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCOCC2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4074092 157065 None 1 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 368 2 0 5 2.3 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCOCC2)CC1 10.1016/j.bmcl.2017.08.043
155539604 172844 None 0 Human Functional pEC50 = 6.2 6.2 2 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4514671 172844 None 0 Human Functional pEC50 = 6.2 6.2 2 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
49674582 156070 None 11 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 2 0 4 4.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4062718 156070 None 11 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 2 0 4 4.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2017.08.043
155539604 172844 None 0 Human Functional pEC50 = 6.2 6.2 2 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4514671 172844 None 0 Human Functional pEC50 = 6.2 6.2 2 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
137647278 157923 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 3 0 5 4.1 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3c(C#N)cnc4ccc(F)cc34)CC1)C2 10.1016/j.bmcl.2017.08.043
CHEMBL4084404 157923 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 3 0 5 4.1 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3c(C#N)cnc4ccc(F)cc34)CC1)C2 10.1016/j.bmcl.2017.08.043
45501063 157208 None 10 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccccc1CNC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4076022 157208 None 10 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccccc1CNC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
49674582 156070 None 11 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 2 0 4 4.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4062718 156070 None 11 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 2 0 4 4.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2017.08.043
156014753 177251 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2n1C 10.1016/j.bmcl.2019.126812
CHEMBL4635969 177251 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2n1C 10.1016/j.bmcl.2019.126812
CHEMBL5086464 215031 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NC3CN(c4ncc(C(F)(F)F)cn4)C3)ncnc12 10.1016/j.bmcl.2021.128416
45501064 156358 None 12 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1 10.1016/j.bmcl.2017.08.043
CHEMBL4065963 156358 None 12 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 418 5 1 5 3.8 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1 10.1016/j.bmcl.2017.08.043
53382516 86317 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313381 86317 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
25067048 12333 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
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 12333 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
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 12333 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
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
71683155 157192 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 7 2.8 Cc1cccc(OC(=O)N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4075751 157192 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 7 2.8 Cc1cccc(OC(=O)N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
162665373 182339 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 425 3 3 9 1.7 Cc1c(O)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4784478 182339 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 425 3 3 9 1.7 Cc1c(O)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
156010821 177064 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126811
156010821 177064 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
CHEMBL4632855 177064 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126811
CHEMBL4632855 177064 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
53382516 86317 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313381 86317 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL5092998 215399 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(C3CCCCC3)ncnc12 10.1016/j.bmcl.2021.128416
3263 4025 None 58 Human Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2018.12.039
864492 4025 None 58 Human Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2018.12.039
CHEMBL1978713 4025 None 58 Human Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2018.12.039
87057213 175753 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 313 3 1 7 3.4 Cc1nnc2sc3c(NCc4ccco4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4583475 175753 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 313 3 1 7 3.4 Cc1nnc2sc3c(NCc4ccco4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
127043638 140426 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 351 3 0 4 4.4 Cc1ccc(OC2CCN(c3cc(C)nc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3809076 140426 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 351 3 0 4 4.4 Cc1ccc(OC2CCN(c3cc(C)nc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
672747 172904 None 13 Rat Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4516088 172904 None 13 Rat Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
127043638 140426 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 351 3 0 4 4.4 Cc1ccc(OC2CCN(c3cc(C)nc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3809076 140426 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 351 3 0 4 4.4 Cc1ccc(OC2CCN(c3cc(C)nc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
672747 172904 None 13 Rat Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4516088 172904 None 13 Rat Functional pEC50 = 6.2 6.2 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 316 2 1 4 4.4 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
155539410 172860 None 0 Human Functional pEC50 = 8.2 8.2 58 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 412 4 0 6 3.4 c1ccc(-n2ccnc2[C@H]2[C@H]3CN(C4CC5(CCN(c6cnccn6)C5)C4)C[C@H]32)cc1 10.1021/acsmedchemlett.9b00106
CHEMBL4515088 172860 None 0 Human Functional pEC50 = 8.2 8.2 58 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 412 4 0 6 3.4 c1ccc(-n2ccnc2[C@H]2[C@H]3CN(C4CC5(CCN(c6cnccn6)C5)C4)C[C@H]32)cc1 10.1021/acsmedchemlett.9b00106
162667825 182515 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 426 3 2 7 3.0 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ccnc(F)c4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4787099 182515 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 426 3 2 7 3.0 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ccnc(F)c4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
56592932 76059 None 1 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 305 3 2 4 3.7 COc1ccc(C)c2sc(NC(=O)NC3CCCC3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057406 76059 None 1 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 305 3 2 4 3.7 COc1ccc(C)c2sc(NC(=O)NC3CCCC3)nc12 10.1016/j.bmcl.2012.05.109
16757564 15281 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 379 3 2 4 4.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(C(F)(F)F)cc3)sc2n1 10.1038/nchembio.2007.55
CHEMBL1212992 15281 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 379 3 2 4 4.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(C(F)(F)F)cc3)sc2n1 10.1038/nchembio.2007.55
89777050 164224 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 2 1 5 3.1 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211076 164224 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 2 1 5 3.1 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89777050 164224 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 2 1 5 3.1 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211076 164224 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 338 2 1 5 3.1 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
156015582 177543 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 3 1 5 3.3 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(F)cc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4640242 177543 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 3 1 5 3.3 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(F)cc2nn1C 10.1016/j.bmcl.2019.126812
137659727 159198 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cnccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4098593 159198 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cnccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
156017640 177822 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1nn(C)c2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc12 10.1016/j.bmcl.2019.126812
CHEMBL4643858 177822 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 1 5 3.2 Cc1nn(C)c2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc12 10.1016/j.bmcl.2019.126812
155540233 172905 None 0 Human Functional pEC50 = 7.1 7.1 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4516136 172905 None 0 Human Functional pEC50 = 7.1 7.1 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
137646732 157792 None 0 Human Functional pEC50 = 7.1 7.1 12 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 422 3 2 7 2.9 Cc1nnc2sc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4083081 157792 None 0 Human Functional pEC50 = 7.1 7.1 12 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 422 3 2 7 2.9 Cc1nnc2sc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
155553146 174077 None 0 Human Functional pEC50 = 7.1 7.1 5 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 424 6 1 8 2.7 Nc1c(C(=O)c2ccncc2)sc2nc(OCCN3CCOCC3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4544318 174077 None 0 Human Functional pEC50 = 7.1 7.1 5 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 424 6 1 8 2.7 Nc1c(C(=O)c2ccncc2)sc2nc(OCCN3CCOCC3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
682264 40210 None 15 Rat Functional pEC50 = 7.1 7.1 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 40210 None 15 Rat Functional pEC50 = 7.1 7.1 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
137646732 157792 None 0 Human Functional pEC50 = 7.1 7.1 12 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 422 3 2 7 2.9 Cc1nnc2sc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4083081 157792 None 0 Human Functional pEC50 = 7.1 7.1 12 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 422 3 2 7 2.9 Cc1nnc2sc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL5083633 214877 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None COCC1CN(c2ncnc3c2sc2nc(C)cc(C)c23)C1 10.1016/j.bmcl.2021.128416
53382542 86313 None 0 Human Functional pEC50 = 7.1 7.1 1 6
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 86313 None 0 Human Functional pEC50 = 7.1 7.1 1 6
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382542 86313 None 0 Human Functional pEC50 = 7.1 7.1 1 6
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 86313 None 0 Human Functional pEC50 = 7.1 7.1 1 6
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89777146 159677 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 2 6 2.1 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104033 159677 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 3 2 6 2.1 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777513 156187 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 421 4 2 6 4.3 Cc1cc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cnc1F 10.1016/j.bmcl.2017.04.043
CHEMBL4064060 156187 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 421 4 2 6 4.3 Cc1cc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cnc1F 10.1016/j.bmcl.2017.04.043
56592911 76121 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 262 3 1 4 2.5 COc1ccc(C)c2sc(C(=O)NC3CC3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057683 76121 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 262 3 1 4 2.5 COc1ccc(C)c2sc(C(=O)NC3CC3)nc12 10.1016/j.bmcl.2012.05.109
137659727 159198 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cnccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4098593 159198 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 355 3 2 8 1.3 Cc1nnc2sc(C(=O)NC3CN(c4cnccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
42598357 16105 None 0 Human Functional pEC50 = 6.1 6.1 -251 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16105 None 0 Human Functional pEC50 = 6.1 6.1 -251 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
25207745 16126 None 0 Human Functional pEC50 = 6.1 6.1 -79 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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 16126 None 0 Human Functional pEC50 = 6.1 6.1 -79 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein 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
134207720 175564 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 2 2 6 3.7 Cc1c(Cl)c2nnc(C)n2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4579086 175564 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 2 2 6 3.7 Cc1c(Cl)c2nnc(C)n2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
137631537 156400 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccncc4Cl)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4066508 156400 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccncc4Cl)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137631537 156400 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccncc4Cl)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4066508 156400 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccncc4Cl)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777239 163953 None 24 Human Functional pEC50 = 7.1 7.1 -1 2
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL4207737 163953 None 24 Human Functional pEC50 = 7.1 7.1 -1 2
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL5268842 163953 None 24 Human Functional pEC50 = 7.1 7.1 -1 2
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1016/j.bmcl.2018.12.039
53382482 86327 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 389 3 2 6 3.8 Cc1nc2sc(C(=O)NCc3ccc4c(c3)OCO4)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313391 86327 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 389 3 2 6 3.8 Cc1nc2sc(C(=O)NCc3ccc4c(c3)OCO4)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382482 86327 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 389 3 2 6 3.8 Cc1nc2sc(C(=O)NCc3ccc4c(c3)OCO4)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313391 86327 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 389 3 2 6 3.8 Cc1nc2sc(C(=O)NCc3ccc4c(c3)OCO4)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382503 86325 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ncccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313389 86325 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ncccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
127043631 140466 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 376 2 0 6 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCSCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809482 140466 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 376 2 0 6 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCSCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
53382503 86325 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ncccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313389 86325 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 347 3 2 6 2.9 Cc1nc2sc(C(=O)NCc3ncccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145974738 164738 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4217609 164738 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
156017866 177903 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 3 2 7 1.6 Cn1nnc2ccc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4644929 177903 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 3 2 7 1.6 Cn1nnc2ccc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
127043631 140466 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 376 2 0 6 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCSCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809482 140466 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 376 2 0 6 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCSCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
156012231 177404 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 268 2 1 6 2.3 Cn1nnc2ccc3c(NC4CCCC4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL4638335 177404 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 268 2 1 6 2.3 Cn1nnc2ccc3c(NC4CCCC4)ncnc3c21 10.1016/j.bmcl.2019.126811
145974738 164738 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4217609 164738 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(C(F)(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
89777468 156527 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 420 5 2 8 3.3 COc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
CHEMBL4067974 156527 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 420 5 2 8 3.3 COc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
134207679 171799 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 4 2 7 3.1 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nc(C)nn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
CHEMBL4468120 171799 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 381 4 2 7 3.1 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nc(C)nn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
89777468 156527 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 420 5 2 8 3.3 COc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
CHEMBL4067974 156527 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 420 5 2 8 3.3 COc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
71792 78406 None 38 Human Functional pEC50 = 6.1 6.1 -2 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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 78406 None 38 Human Functional pEC50 = 6.1 6.1 -2 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 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
53382544 86322 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313386 86322 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156020885 178163 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 281 2 1 5 3.2 Cc1c2c(ccc3c(NC4CCCC4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4649056 178163 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 281 2 1 5 3.2 Cc1c2c(ccc3c(NC4CCCC4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
156013305 177492 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.7 Cc1nc2ncc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4639394 177492 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.7 Cc1nc2ncc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL5078961 214596 None 1 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NC3CCC3)nccc12 10.1016/j.bmcl.2021.128416
30299339 140386 None 2 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 444 4 1 7 3.6 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(C)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808592 140386 None 2 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 444 4 1 7 3.6 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(C)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
145965320 164357 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1cccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.10.053
CHEMBL4212735 164357 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1cccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.10.053
145965320 164357 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1cccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.10.053
CHEMBL4212735 164357 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1cccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.10.053
30299339 140386 None 2 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 444 4 1 7 3.6 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(C)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808592 140386 None 2 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 444 4 1 7 3.6 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(C)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
53382544 86322 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313386 86322 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145978470 163602 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 3 1 3 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203579 163602 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 3 1 3 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
145978470 163602 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 3 1 3 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203579 163602 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 3 1 3 3.7 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
122195090 124097 None 0 Human Functional pEC50 = 7.1 7.1 -6 2
Partial agonist activity at human muscarinic M4 acetylcholine receptor expressed in CHO cells co-expressing Galpha16 assessed as calcium mobilization by FLIPR assayPartial agonist activity at human muscarinic M4 acetylcholine receptor expressed in CHO cells co-expressing Galpha16 assessed as calcium mobilization by FLIPR assay
ChEMBL 412 4 1 4 3.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@@H](N3Cc4ccccc4NC3=O)C1)C2 10.1016/j.bmcl.2015.09.032
CHEMBL3633184 124097 None 0 Human Functional pEC50 = 7.1 7.1 -6 2
Partial agonist activity at human muscarinic M4 acetylcholine receptor expressed in CHO cells co-expressing Galpha16 assessed as calcium mobilization by FLIPR assayPartial agonist activity at human muscarinic M4 acetylcholine receptor expressed in CHO cells co-expressing Galpha16 assessed as calcium mobilization by FLIPR assay
ChEMBL 412 4 1 4 3.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@@H](N3Cc4ccccc4NC3=O)C1)C2 10.1016/j.bmcl.2015.09.032
155521109 170540 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 364 2 2 7 2.1 Cc1cc2ncnn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4449879 170540 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 364 2 2 7 2.1 Cc1cc2ncnn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
137653737 158694 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccccn2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4093138 158694 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccccn2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL5077425 214499 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(OCc3ccc(C(C)(C)O)cc3)ncnc12 10.1016/j.bmcl.2021.128416
156013700 177275 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 361 4 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4636269 177275 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 361 4 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4640311 177275 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 361 4 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
134207687 173433 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 4 2 7 2.8 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nncn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
CHEMBL4528914 173433 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 4 2 7 2.8 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nncn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
683024 51306 None 24 Human Functional pEC50 = 6.1 6.1 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL1581020 51306 None 24 Human Functional pEC50 = 6.1 6.1 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
155560153 174951 None 0 Human Functional pEC50 = 6.1 6.1 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4565738 174951 None 0 Human Functional pEC50 = 6.1 6.1 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
683024 51306 None 24 Human Functional pEC50 = 6.1 6.1 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL1581020 51306 None 24 Human Functional pEC50 = 6.1 6.1 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
155560153 174951 None 0 Human Functional pEC50 = 6.1 6.1 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4565738 174951 None 0 Human Functional pEC50 = 6.1 6.1 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3ccncc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
45501061 156775 None 12 Human Functional pEC50 = 6.1 6.1 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4070787 156775 None 12 Human Functional pEC50 = 6.1 6.1 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
155552304 174040 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 5 3.3 CCOC(=O)N1CCC2(CC(N3CCC(c4ncccc4OC)CC3)C2)C1 10.1021/acsmedchemlett.9b00106
CHEMBL4543638 174040 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 5 3.3 CCOC(=O)N1CCC2(CC(N3CCC(c4ncccc4OC)CC3)C2)C1 10.1021/acsmedchemlett.9b00106
302 2977 None 25 Human Functional pEC50 = 8.1 8.1 1 8
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
4630 2977 None 25 Human Functional pEC50 = 8.1 8.1 1 8
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
CHEMBL7634 2977 None 25 Human Functional pEC50 = 8.1 8.1 1 8
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
44589681 185288 None 0 Human Functional pEC50 = 8.0 8.0 1 5
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 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 185288 None 0 Human Functional pEC50 = 8.0 8.0 1 5
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 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 187063 None 1 Human Functional pEC50 = 8.0 8.0 -4 5
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 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 187063 None 1 Human Functional pEC50 = 8.0 8.0 -4 5
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 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
134263768 183141 None 7 Human Functional pEC50 = 7.1 7.1 -3 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 439 4 2 9 2.0 COc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4795177 183141 None 7 Human Functional pEC50 = 7.1 7.1 -3 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 439 4 2 9 2.0 COc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
162674698 183289 None 0 Human Functional pEC50 = 7.1 7.1 12 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 423 3 2 8 2.3 Cc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4796921 183289 None 0 Human Functional pEC50 = 7.1 7.1 12 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 423 3 2 8 2.3 Cc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
137646585 158000 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 0 5 4.5 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(Cl)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4085356 158000 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 0 5 4.5 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(Cl)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
12301 4047 None 30 Human Functional pEC50 = 7.0 7.0 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.053
73774630 4047 None 30 Human Functional pEC50 = 7.0 7.0 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.053
CHEMBL3915634 4047 None 30 Human Functional pEC50 = 7.0 7.0 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2017.10.053
89777151 158573 None 0 Human Functional pEC50 = 7.0 7.0 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4091821 158573 None 0 Human Functional pEC50 = 7.0 7.0 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
156020012 178096 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 3 2 7 1.9 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4647876 178096 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 391 3 2 7 1.9 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
137635723 156083 None 0 Human Functional pEC50 = 7.0 7.0 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062934 156083 None 0 Human Functional pEC50 = 7.0 7.0 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777151 158573 None 0 Human Functional pEC50 = 7.0 7.0 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4091821 158573 None 0 Human Functional pEC50 = 7.0 7.0 -7 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5074747 214331 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc(C(C)(C)O)cc3)ncnc12 10.1016/j.bmcl.2021.128416
137653737 158694 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccccn2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4093138 158694 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccccn2)CC1 10.1016/j.bmcl.2017.08.043
137646585 158000 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 0 5 4.5 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(Cl)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4085356 158000 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 0 5 4.5 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(Cl)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
53382541 86309 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 366 4 2 5 3.4 Cc1nc2sc(C(=O)NCCC3CCCN3C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313373 86309 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 366 4 2 5 3.4 Cc1nc2sc(C(=O)NCCC3CCCN3C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
73672762 112024 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Agonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 436 4 0 6 2.1 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
CHEMBL3289440 112024 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Agonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 436 4 0 6 2.1 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
137645044 158104 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 485 4 2 8 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4086665 158104 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 485 4 2 8 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137657309 159611 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.9 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncn2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4103312 159611 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.9 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncn2)CC1 10.1016/j.bmcl.2017.08.043
53382541 86309 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 366 4 2 5 3.4 Cc1nc2sc(C(=O)NCCC3CCCN3C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313373 86309 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 366 4 2 5 3.4 Cc1nc2sc(C(=O)NCCC3CCCN3C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145963925 164327 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncccc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4212428 164327 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncccc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137645044 158104 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 485 4 2 8 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4086665 158104 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 485 4 2 8 2.8 Cc1nnc2sc(C(=O)NC3CN(c4ccc(S(=O)(=O)C(F)(F)F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
145963925 164327 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncccc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4212428 164327 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ncccc4Cl)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137657309 159611 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.9 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncn2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4103312 159611 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 3 1 6 2.9 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncn2)CC1 10.1016/j.bmcl.2017.08.043
156009865 177110 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 439 4 1 6 3.3 COc1cc(N2CC(NC(=O)c3ccc4nc(C(F)(F)F)n(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4633549 177110 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 439 4 1 6 3.3 COc1cc(N2CC(NC(=O)c3ccc4nc(C(F)(F)F)n(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
155547285 173623 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 4 2 7 2.8 COc1ccc(CNC(=O)c2sc3c(c(C)cc4ncnn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
CHEMBL4533756 173623 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 367 4 2 7 2.8 COc1ccc(CNC(=O)c2sc3c(c(C)cc4ncnn43)c2N)cc1 10.1016/j.bmcl.2019.06.032
45142486 52359 None 0 Rat Functional pEC50 = 7.0 7.0 -2 2
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 nan
CHEMBL1589763 52359 None 0 Rat Functional pEC50 = 7.0 7.0 -2 2
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 nan
127044078 140375 None 0 Rat Functional pEC50 = 6.0 6.0 1 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3808485 140375 None 0 Rat Functional pEC50 = 6.0 6.0 1 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 338 3 0 5 3.5 Cc1ccc(OC2CCN(c3ncnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2016.05.010
55661332 140455 None 4 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 484 3 0 7 3.9 Cc1sc2ncnc(N3CCC(C(=O)N4CCCc5cc(S(C)(=O)=O)ccc54)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809378 140455 None 4 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 484 3 0 7 3.9 Cc1sc2ncnc(N3CCC(C(=O)N4CCCc5cc(S(C)(=O)=O)ccc54)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
156010835 177090 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 416 5 2 6 4.2 Cc1c2c(ccc3c(NCc4ccc(C(=O)NCC(C)(C)C)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4633191 177090 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 416 5 2 6 4.2 Cc1c2c(ccc3c(NCc4ccc(C(=O)NCC(C)(C)C)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
55661332 140455 None 4 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 484 3 0 7 3.9 Cc1sc2ncnc(N3CCC(C(=O)N4CCCc5cc(S(C)(=O)=O)ccc54)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809378 140455 None 4 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 484 3 0 7 3.9 Cc1sc2ncnc(N3CCC(C(=O)N4CCCc5cc(S(C)(=O)=O)ccc54)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
145975851 163729 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(Cl)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4205221 163729 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(Cl)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
127044539 140419 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 362 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CC[C@H](F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808983 140419 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 362 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CC[C@H](F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
127044539 140419 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 362 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CC[C@H](F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808983 140419 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 362 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CC[C@H](F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
145975851 163729 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(Cl)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4205221 163729 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 366 3 1 4 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(Cl)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
155561871 175825 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3cncc(C)n3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4584879 175825 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 381 4 0 6 3.4 COc1cccnc1C1CCN(C2CCCN(c3cncc(C)n3)CC2)CC1 10.1021/acsmedchemlett.9b00106
44626302 48143 None 0 Rat Functional pEC50 = 7 7.0 - 1
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 434 7 2 7 4.1 COc1ccc(CNC(=O)c2sc3nc(OCc4ccncc4)cc(C)c3c2N)cc1 nan
CHEMBL1551487 48143 None 0 Rat Functional pEC50 = 7 7.0 - 1
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 434 7 2 7 4.1 COc1ccc(CNC(=O)c2sc3nc(OCc4ccncc4)cc(C)c3c2N)cc1 nan
155531483 171678 None 0 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 469 4 2 8 3.1 Cc1cc2nncn2c2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4466365 171678 None 0 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 469 4 2 8 3.1 Cc1cc2nncn2c2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
89777513 156187 None 0 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 421 4 2 6 4.3 Cc1cc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cnc1F 10.1016/j.bmcl.2017.04.043
CHEMBL4064060 156187 None 0 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 421 4 2 6 4.3 Cc1cc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cnc1F 10.1016/j.bmcl.2017.04.043
2551 794 None 23 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
2551.0 794 None 23 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 794 None 23 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 794 None 23 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 794 None 23 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 794 None 23 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
9795428 96488 None 5 Human Functional pED50 = 7.3 7.3 -1 5
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 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 96488 None 5 Human Functional pED50 = 7.3 7.3 -1 5
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 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
5487543 205646 None 4 Human Functional pED50 = 7.0 7.0 1 6
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
CHEMBL81878 205646 None 4 Human Functional pED50 = 7.0 7.0 1 6
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
138578326 186228 None 0 Human Functional pIC50 = 9.4 9.4 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4861863 186228 None 0 Human Functional pIC50 = 9.4 9.4 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873386 186228 None 0 Human Functional pIC50 = 9.4 9.4 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578326 186228 None 0 Human Functional pIC50 = 9.4 9.4 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4861863 186228 None 0 Human Functional pIC50 = 9.4 9.4 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873386 186228 None 0 Human Functional pIC50 = 9.4 9.4 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578326 186228 None 0 Human Functional pIC50 = 9.2 9.2 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4861863 186228 None 0 Human Functional pIC50 = 9.2 9.2 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873386 186228 None 0 Human Functional pIC50 = 9.2 9.2 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578326 186228 None 0 Human Functional pIC50 = 9.2 9.2 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4861863 186228 None 0 Human Functional pIC50 = 9.2 9.2 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873386 186228 None 0 Human Functional pIC50 = 9.2 9.2 870 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
156493644 185062 None 0 Human Functional pIC50 = 8.8 8.8 1737 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 435 6 2 6 3.7 CC(=O)Nc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4855467 185062 None 0 Human Functional pIC50 = 8.8 8.8 1737 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 435 6 2 6 3.7 CC(=O)Nc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
156493644 185062 None 0 Human Functional pIC50 = 8.8 8.8 1737 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 435 6 2 6 3.7 CC(=O)Nc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4855467 185062 None 0 Human Functional pIC50 = 8.8 8.8 1737 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 435 6 2 6 3.7 CC(=O)Nc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
138578970 185667 None 0 Human Functional pIC50 = 8.8 8.8 1862 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 414 5 1 5 4.0 Fc1ccc(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4864914 185667 None 0 Human Functional pIC50 = 8.8 8.8 1862 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 414 5 1 5 4.0 Fc1ccc(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578970 185667 None 0 Human Functional pIC50 = 8.8 8.8 1862 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 414 5 1 5 4.0 Fc1ccc(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4864914 185667 None 0 Human Functional pIC50 = 8.8 8.8 1862 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 414 5 1 5 4.0 Fc1ccc(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578683 184803 None 0 Human Functional pIC50 = 8.8 8.8 1318 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccccc1-c1ccc(N[C@H]2C[C@@H]3CN(CC4CCOCC4)C[C@@H]3C2)nn1 10.1021/acsmedchemlett.1c00363
CHEMBL4851711 184803 None 0 Human Functional pIC50 = 8.8 8.8 1318 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccccc1-c1ccc(N[C@H]2C[C@@H]3CN(CC4CCOCC4)C[C@@H]3C2)nn1 10.1021/acsmedchemlett.1c00363
137408729 190742 None 0 Human Functional pIC50 = 8.7 8.7 870 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 444 6 1 5 4.9 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5182783 190742 None 0 Human Functional pIC50 = 8.7 8.7 870 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 444 6 1 5 4.9 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137408729 190742 None 0 Human Functional pIC50 = 8.7 8.7 870 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 444 6 1 5 4.9 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5182783 190742 None 0 Human Functional pIC50 = 8.7 8.7 870 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 444 6 1 5 4.9 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137637944 155815 None 0 Human Functional pIC50 = 7 7.0 2 5
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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 155815 None 0 Human Functional pIC50 = 7 7.0 2 5
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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
52176747 159031 None 1 Rat Functional pIC50 = 6 6.0 -2 8
Antagonist activity at rat muscarinic M4 receptor by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor 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 159031 None 1 Rat Functional pIC50 = 6 6.0 -2 8
Antagonist activity at rat muscarinic M4 receptor by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor 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
137634235 156651 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4069356 156651 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
156015807 178299 None 0 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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 178299 None 0 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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 178299 None 0 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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
137634235 156651 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4069356 156651 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137638270 156877 None 0 Human Functional pIC50 = 7.0 7.0 2 5
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 156877 None 0 Human Functional pIC50 = 7.0 7.0 2 5
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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
9815331 203107 None 1 Rat Functional pIC50 = 8.0 8.0 -3 5
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 203107 None 1 Rat Functional pIC50 = 8.0 8.0 -3 5
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
152072967 192238 None 0 Human Functional pIC50 = 7.9 7.9 6 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5205163 192238 None 0 Human Functional pIC50 = 7.9 7.9 6 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137641287 157048 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 452 4 0 7 2.9 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4ncccc4c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4073915 157048 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 452 4 0 7 2.9 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4ncccc4c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137658248 159625 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 466 4 0 5 4.9 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4103428 159625 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 466 4 0 5 4.9 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137641287 157048 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 452 4 0 7 2.9 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4ncccc4c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4073915 157048 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 452 4 0 7 2.9 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4ncccc4c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
152072967 192238 None 0 Human Functional pIC50 = 7.9 7.9 6 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5205163 192238 None 0 Human Functional pIC50 = 7.9 7.9 6 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
9913341 82158 None 4 Human Functional pIC50 = 7.9 7.9 -28 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 82158 None 4 Human Functional pIC50 = 7.9 7.9 -28 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL553058 82158 None 4 Human Functional pIC50 = 7.9 7.9 -28 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
137638270 156877 None 0 Human Functional pIC50 = 6.9 6.9 2 5
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 156877 None 0 Human Functional pIC50 = 6.9 6.9 2 5
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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
168279172 190899 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 392 6 1 5 4.1 c1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5185022 190899 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 392 6 1 5 4.1 c1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
137655063 158973 None 0 Human Functional pIC50 = 6.9 6.9 2 5
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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 158973 None 0 Human Functional pIC50 = 6.9 6.9 2 5
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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
168279172 190899 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 392 6 1 5 4.1 c1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5185022 190899 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 392 6 1 5 4.1 c1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
168289751 191810 None 0 Human Functional pIC50 = 6.9 6.9 47 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 7 4.0 Cn1cc2cc(-c3ccc(NC[C@@H]4CC45CCN(CC4CCOCC4)CC5)nn3)ccc2n1 10.1016/j.bmcl.2021.128479
CHEMBL5198423 191810 None 0 Human Functional pIC50 = 6.9 6.9 47 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 7 4.0 Cn1cc2cc(-c3ccc(NC[C@@H]4CC45CCN(CC4CCOCC4)CC5)nn3)ccc2n1 10.1016/j.bmcl.2021.128479
44418764 82159 None 0 Human Functional pIC50 = 5.9 5.9 -5 4
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 82159 None 0 Human Functional pIC50 = 5.9 5.9 -5 4
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
121053110 158506 None 1 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4091144 158506 None 1 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
121053110 158506 None 1 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4091144 158506 None 1 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
137655063 158973 None 0 Human Functional pIC50 = 6.9 6.9 2 5
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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 158973 None 0 Human Functional pIC50 = 6.9 6.9 2 5
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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
168289751 191810 None 0 Human Functional pIC50 = 6.9 6.9 47 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 7 4.0 Cn1cc2cc(-c3ccc(NC[C@@H]4CC45CCN(CC4CCOCC4)CC5)nn3)ccc2n1 10.1016/j.bmcl.2021.128479
CHEMBL5198423 191810 None 0 Human Functional pIC50 = 6.9 6.9 47 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 7 4.0 Cn1cc2cc(-c3ccc(NC[C@@H]4CC45CCN(CC4CCOCC4)CC5)nn3)ccc2n1 10.1016/j.bmcl.2021.128479
137647734 157846 None 0 Human Functional pIC50 = 6.9 6.9 2 5
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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 157846 None 0 Human Functional pIC50 = 6.9 6.9 2 5
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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
137660952 159347 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 443 4 0 6 3.3 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2017.05.042
CHEMBL4100202 159347 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 443 4 0 6 3.3 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2017.05.042
137655354 158638 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 444 4 0 7 2.7 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nc1 10.1016/j.bmcl.2017.05.042
CHEMBL4092457 158638 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 444 4 0 7 2.7 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nc1 10.1016/j.bmcl.2017.05.042
156016041 178247 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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 178247 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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 178247 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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
71451570 81948 None 0 Human Functional pIC50 = 6.9 6.9 -7 3
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
ChEMBL 326 4 0 2 2.9 CN1CCN(C(=O)[C@@](F)(Cc2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2012.09.011
CHEMBL2164905 81948 None 0 Human Functional pIC50 = 6.9 6.9 -7 3
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
ChEMBL 326 4 0 2 2.9 CN1CCN(C(=O)[C@@](F)(Cc2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2012.09.011
137647734 157846 None 0 Human Functional pIC50 = 6.9 6.9 2 5
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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 157846 None 0 Human Functional pIC50 = 6.9 6.9 2 5
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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
137658248 159625 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 466 4 0 5 4.9 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4103428 159625 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 466 4 0 5 4.9 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
127045035 140412 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayAntagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 6 0 6 5.3 CCCCN(c1ccc(C)nc1)C1CCN(c2ncnc3sc(C)c(C)c23)CC1 10.1016/j.bmcl.2016.05.010
CHEMBL3808906 140412 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayAntagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 409 6 0 6 5.3 CCCCN(c1ccc(C)nc1)C1CCN(c2ncnc3sc(C)c(C)c23)CC1 10.1016/j.bmcl.2016.05.010
46830362 7894 None 0 Human Functional pIC50 = 5.8 5.8 -3 5
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein 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 7894 None 0 Human Functional pIC50 = 5.8 5.8 -3 5
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein 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
11584660 93268 None 8 Human Functional pIC50 = 6.8 6.8 1 5
Antagonist activity at human muscarinic receptor M4Antagonist activity at human muscarinic receptor M4
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL244946 93268 None 8 Human Functional pIC50 = 6.8 6.8 1 5
Antagonist activity at human muscarinic receptor M4Antagonist activity at human muscarinic receptor M4
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
137641843 158261 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 405 4 0 8 1.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3nccn3C)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4088672 158261 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 405 4 0 8 1.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3nccn3C)CC2)nn1 10.1016/j.bmcl.2017.05.042
137641843 158261 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 405 4 0 8 1.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3nccn3C)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4088672 158261 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 405 4 0 8 1.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3nccn3C)CC2)nn1 10.1016/j.bmcl.2017.05.042
137658023 159715 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cccc(F)c3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4104456 159715 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cccc(F)c3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137408799 190940 None 0 Human Functional pIC50 = 7.8 7.8 12 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NCC3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5185664 190940 None 0 Human Functional pIC50 = 7.8 7.8 12 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NCC3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
2986945 95055 None 7 Rat Functional pIC50 = 4.8 4.8 -16 5
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 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 95055 None 7 Rat Functional pIC50 = 4.8 4.8 -16 5
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 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
152278786 182752 None 1 Human Functional pIC50 = 7.7 7.7 -12 4
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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 182752 None 1 Human Functional pIC50 = 7.7 7.7 -12 4
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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
137658023 159715 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cccc(F)c3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4104456 159715 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cccc(F)c3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137649829 157419 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4078634 157419 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
156493565 184986 None 0 Human Functional pIC50 = 8.6 8.6 1318 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1cccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4854289 184986 None 0 Human Functional pIC50 = 8.6 8.6 1318 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1cccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
156493565 184986 None 0 Human Functional pIC50 = 8.6 8.6 1318 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1cccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4854289 184986 None 0 Human Functional pIC50 = 8.6 8.6 1318 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1cccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578253 186455 None 0 Human Functional pIC50 = 8.6 8.6 1230 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 378 5 1 5 3.7 c1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4876599 186455 None 0 Human Functional pIC50 = 8.6 8.6 1230 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 378 5 1 5 3.7 c1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
138578253 186455 None 0 Human Functional pIC50 = 8.6 8.6 1230 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 378 5 1 5 3.7 c1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4876599 186455 None 0 Human Functional pIC50 = 8.6 8.6 1230 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 378 5 1 5 3.7 c1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
137649829 157419 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4078634 157419 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
44455159 97765 None 0 Rat Functional pIC50 = 4.7 4.7 -17 5
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 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 97765 None 0 Rat Functional pIC50 = 4.7 4.7 -17 5
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 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
152278786 182752 None 1 Human Functional pIC50 = 7.7 7.7 -12 4
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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 182752 None 1 Human Functional pIC50 = 7.7 7.7 -12 4
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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
137408799 190940 None 0 Rat Functional pIC50 = 6.6 6.6 -12 2
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NCC3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5185664 190940 None 0 Rat Functional pIC50 = 6.6 6.6 -12 2
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NCC3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137655902 158820 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccc(F)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4094531 158820 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccc(F)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137639216 156708 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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)c3ccc(Cl)cc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4070135 156708 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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)c3ccc(Cl)cc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
2551 794 None 23 Rat Functional pIC50 = 6.6 6.6 -2 13
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
2551.0 794 None 23 Rat Functional pIC50 = 6.6 6.6 -2 13
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
298 794 None 23 Rat Functional pIC50 = 6.6 6.6 -2 13
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
488 794 None 23 Rat Functional pIC50 = 6.6 6.6 -2 13
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
CHEMBL965 794 None 23 Rat Functional pIC50 = 6.6 6.6 -2 13
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
DB00411 794 None 23 Rat Functional pIC50 = 6.6 6.6 -2 13
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
137639216 156708 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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)c3ccc(Cl)cc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4070135 156708 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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)c3ccc(Cl)cc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137647376 157591 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 5 0 7 2.4 COc1ccccc1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4080796 157591 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 5 0 7 2.4 COc1ccccc1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
137647376 157591 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 5 0 7 2.4 COc1ccccc1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4080796 157591 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 5 0 7 2.4 COc1ccccc1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
137635985 156078 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)CC2 10.1016/j.bmcl.2017.04.009
CHEMBL4062851 156078 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)CC2 10.1016/j.bmcl.2017.04.009
137655902 158820 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccc(F)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4094531 158820 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccc(F)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
127045185 140414 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayAntagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 395 5 0 6 4.9 CCCN(c1ccc(C)nc1)C1CCN(c2ncnc3sc(C)c(C)c23)CC1 10.1016/j.bmcl.2016.05.010
CHEMBL3808947 140414 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayAntagonist activity at human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 395 5 0 6 4.9 CCCN(c1ccc(C)nc1)C1CCN(c2ncnc3sc(C)c(C)c23)CC1 10.1016/j.bmcl.2016.05.010
137635985 156078 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)CC2 10.1016/j.bmcl.2017.04.009
CHEMBL4062851 156078 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)CC2 10.1016/j.bmcl.2017.04.009
3652 4097 None 79 Human Functional pIC50 = 7.6 7.6 -8 15
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4097 None 79 Human Functional pIC50 = 7.6 7.6 -8 15
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4097 None 79 Human Functional pIC50 = 7.6 7.6 -8 15
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809.0 4097 None 79 Human Functional pIC50 = 7.6 7.6 -8 15
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4097 None 79 Human Functional pIC50 = 7.6 7.6 -8 15
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4097 None 79 Human Functional pIC50 = 7.6 7.6 -8 15
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
162646559 179640 None 0 Human Functional pIC50 = 6.6 6.6 -19 4
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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 179640 None 0 Human Functional pIC50 = 6.6 6.6 -19 4
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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
10109893 82165 None 0 Human Functional pIC50 = 4.6 4.6 -3162 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
CHEMBL216983 82165 None 0 Human Functional pIC50 = 4.6 4.6 -3162 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
CHEMBL544840 82165 None 0 Human Functional pIC50 = 4.6 4.6 -3162 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
137659030 159225 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 401 4 0 6 2.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4098838 159225 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 401 4 0 6 2.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137659030 159225 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 401 4 0 6 2.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4098838 159225 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 401 4 0 6 2.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137658151 159708 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4104377 159708 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
137654928 158702 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 482 4 0 5 5.4 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3Cl)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4093252 158702 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 482 4 0 5 5.4 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3Cl)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137655967 159024 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 461 6 0 8 2.4 COc1ccc(S(=O)(=O)N2CCN(c3ccc(N4CCCC[C@@H]4C)nn3)CC2)cc1OC 10.1016/j.bmcl.2017.05.042
CHEMBL4096649 159024 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 461 6 0 8 2.4 COc1ccc(S(=O)(=O)N2CCN(c3ccc(N4CCCC[C@@H]4C)nn3)CC2)cc1OC 10.1016/j.bmcl.2017.05.042
137648504 158011 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3c(F)cccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4085498 158011 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3c(F)cccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137408797 190448 None 0 Human Functional pIC50 = 7.6 7.6 18 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5178468 190448 None 0 Human Functional pIC50 = 7.6 7.6 18 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137654928 158702 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 482 4 0 5 5.4 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3Cl)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4093252 158702 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 482 4 0 5 5.4 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3Cl)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137648504 158011 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3c(F)cccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4085498 158011 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3c(F)cccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137658151 159708 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4104377 159708 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccc4c(c3)OCO4)CC2)nn1 10.1016/j.bmcl.2017.05.042
168294040 192193 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5204478 192193 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
137408797 190448 None 0 Human Functional pIC50 = 7.6 7.6 18 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5178468 190448 None 0 Human Functional pIC50 = 7.6 7.6 18 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
168294040 192193 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5204478 192193 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
137655967 159024 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 461 6 0 8 2.4 COc1ccc(S(=O)(=O)N2CCN(c3ccc(N4CCCC[C@@H]4C)nn3)CC2)cc1OC 10.1016/j.bmcl.2017.05.042
CHEMBL4096649 159024 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 461 6 0 8 2.4 COc1ccc(S(=O)(=O)N2CCN(c3ccc(N4CCCC[C@@H]4C)nn3)CC2)cc1OC 10.1016/j.bmcl.2017.05.042
137661476 159459 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4101349 159459 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
137644574 158088 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4086480 158088 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
142611618 191192 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 416 5 1 5 4.2 Fc1ccc(Cl)c(-c2ccc(NC3CC4(C3)CN(CC3CCOCC3)C4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5189221 191192 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 416 5 1 5 4.2 Fc1ccc(Cl)c(-c2ccc(NC3CC4(C3)CN(CC3CCOCC3)C4)nn2)c1 10.1016/j.bmcl.2021.128479
137661476 159459 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4101349 159459 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 445 4 0 8 2.1 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
137644574 158088 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4086480 158088 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 C[C@H]1CCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
142611618 191192 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 416 5 1 5 4.2 Fc1ccc(Cl)c(-c2ccc(NC3CC4(C3)CN(CC3CCOCC3)C4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5189221 191192 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 416 5 1 5 4.2 Fc1ccc(Cl)c(-c2ccc(NC3CC4(C3)CN(CC3CCOCC3)C4)nn2)c1 10.1016/j.bmcl.2021.128479
137636810 155916 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3cccc(F)c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4060844 155916 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3cccc(F)c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137648177 157832 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 428 4 0 5 4.4 Cc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4083448 157832 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 428 4 0 5 4.4 Cc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
137636810 155916 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3cccc(F)c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4060844 155916 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3cccc(F)c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137648177 157832 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 428 4 0 5 4.4 Cc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4083448 157832 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 428 4 0 5 4.4 Cc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
53303986 74340 None 0 Human Functional pIC50 = 5.5 5.5 -20 3
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024407 74340 None 0 Human Functional pIC50 = 5.5 5.5 -20 3
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
137654353 159016 None 0 Human Functional pIC50 = 6.5 6.5 1 6
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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 159016 None 0 Human Functional pIC50 = 6.5 6.5 1 6
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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
168276820 190106 None 0 Human Functional pIC50 = 7.5 7.5 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5172967 190106 None 0 Human Functional pIC50 = 7.5 7.5 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5208649 190106 None 0 Human Functional pIC50 = 7.5 7.5 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
168276820 190106 None 0 Human Functional pIC50 = 7.5 7.5 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5172967 190106 None 0 Human Functional pIC50 = 7.5 7.5 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5208649 190106 None 0 Human Functional pIC50 = 7.5 7.5 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137641912 158383 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 406 4 0 8 1.6 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4089875 158383 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 406 4 0 8 1.6 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
137641912 158383 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 406 4 0 8 1.6 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4089875 158383 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 406 4 0 8 1.6 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
137654353 159016 None 0 Human Functional pIC50 = 6.5 6.5 1 6
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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 159016 None 0 Human Functional pIC50 = 6.5 6.5 1 6
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 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
49663949 158031 None 10 Human Functional pIC50 = 6.5 6.5 1 2
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4085711 158031 None 10 Human Functional pIC50 = 6.5 6.5 1 2
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
156015978 178323 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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 178323 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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 178323 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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
46883796 7893 None 0 Human Functional pIC50 = 5.4 5.4 -1 4
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein 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 7893 None 0 Human Functional pIC50 = 5.4 5.4 -1 4
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein 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
46830363 8019 None 0 Human Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090759 8019 None 0 Human Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
1421986 8265 None 4 Human Functional pIC50 = 5.4 5.4 -1 3
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 357 4 1 3 4.0 CCN1CCN(c2ccc(NC(=O)c3ccc(C)cc3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1092461 8265 None 4 Human Functional pIC50 = 5.4 5.4 -1 3
Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 357 4 1 3 4.0 CCN1CCN(c2ccc(NC(=O)c3ccc(C)cc3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
49663949 158031 None 10 Human Functional pIC50 = 6.4 6.4 1 2
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4085711 158031 None 10 Human Functional pIC50 = 6.4 6.4 1 2
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
162657046 180843 None 0 Human Functional pIC50 = 7.4 7.4 -6 4
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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 180843 None 0 Human Functional pIC50 = 7.4 7.4 -6 4
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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
16094788 141915 None 0 Human Functional pIC50 = 6.4 6.4 -1 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL386983 141915 None 0 Human Functional pIC50 = 6.4 6.4 -1 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
137634274 156507 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 407 4 0 6 2.6 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)C3CCCCC3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4067738 156507 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 407 4 0 6 2.6 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)C3CCCCC3)CC2)nn1 10.1016/j.bmcl.2017.05.042
164606754 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4850236 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873617 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
164606754 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4850236 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873617 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
164606754 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4850236 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873617 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
164606754 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4850236 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873617 184702 None 7 Human Functional pIC50 = 8.4 8.4 33 3
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
137634274 156507 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 407 4 0 6 2.6 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)C3CCCCC3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4067738 156507 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 407 4 0 6 2.6 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)C3CCCCC3)CC2)nn1 10.1016/j.bmcl.2017.05.042
121053122 157824 None 1 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4083366 157824 None 1 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
137647522 157936 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 456 4 0 5 4.8 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCC2CCCCC2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4084528 157936 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 456 4 0 5 4.8 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCC2CCCCC2C1 10.1016/j.bmcl.2017.04.009
168276820 190106 None 0 Human Functional pIC50 = 7.4 7.4 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5172967 190106 None 0 Human Functional pIC50 = 7.4 7.4 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5208649 190106 None 0 Human Functional pIC50 = 7.4 7.4 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137647522 157936 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 456 4 0 5 4.8 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCC2CCCCC2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4084528 157936 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 456 4 0 5 4.8 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCC2CCCCC2C1 10.1016/j.bmcl.2017.04.009
168276820 190106 None 0 Human Functional pIC50 = 7.4 7.4 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5172967 190106 None 0 Human Functional pIC50 = 7.4 7.4 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5208649 190106 None 0 Human Functional pIC50 = 7.4 7.4 63 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
52176747 159031 None 1 Human Functional pIC50 = 6.4 6.4 2 8
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 159031 None 1 Human Functional pIC50 = 6.4 6.4 2 8
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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
121053122 157824 None 1 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4083366 157824 None 1 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
52176747 159031 None 1 Human Functional pIC50 = 6.4 6.4 2 8
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 159031 None 1 Human Functional pIC50 = 6.4 6.4 2 8
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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
137636570 155887 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 459 4 0 8 2.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccc5c(c4)OCO5)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
CHEMBL4060501 155887 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 459 4 0 8 2.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccc5c(c4)OCO5)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
137635323 156146 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 444 5 0 6 4.1 COc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4063633 156146 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 444 5 0 6 4.1 COc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
137636570 155887 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 459 4 0 8 2.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccc5c(c4)OCO5)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
CHEMBL4060501 155887 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 459 4 0 8 2.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccc5c(c4)OCO5)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
9308 17754 None 21 Rat Functional pIC50 = 6.3 6.3 -3 9
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
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 17754 None 21 Rat Functional pIC50 = 6.3 6.3 -3 9
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
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 17754 None 21 Rat Functional pIC50 = 6.3 6.3 -3 9
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
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 17754 None 21 Rat Functional pIC50 = 6.3 6.3 -3 9
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
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
137654353 159016 None 0 Rat Functional pIC50 = 6.3 6.3 -1 6
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor 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 159016 None 0 Rat Functional pIC50 = 6.3 6.3 -1 6
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor 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
10092649 193073 None 56 Rat Functional pIC50 = 6.3 6.3 -6 11
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 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 193073 None 56 Rat Functional pIC50 = 6.3 6.3 -6 11
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 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 193073 None 56 Rat Functional pIC50 = 6.3 6.3 -6 11
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 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 193073 None 56 Rat Functional pIC50 = 6.3 6.3 -6 11
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 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
1201549 597 None 24 Human Functional pIC50 = 8.3 8.3 -1 26
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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
1201549.0 597 None 24 Human Functional pIC50 = 8.3 8.3 -1 26
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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
333 597 None 24 Human Functional pIC50 = 8.3 8.3 -1 26
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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 597 None 24 Human Functional pIC50 = 8.3 8.3 -1 26
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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 597 None 24 Human Functional pIC50 = 8.3 8.3 -1 26
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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 597 None 24 Human Functional pIC50 = 8.3 8.3 -1 26
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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 597 None 24 Human Functional pIC50 = 8.3 8.3 -1 26
Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M4 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
138578974 184598 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 379 5 1 6 3.1 c1cncc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4848896 184598 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 379 5 1 6 3.1 c1cncc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
138578974 184598 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 379 5 1 6 3.1 c1cncc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4848896 184598 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 379 5 1 6 3.1 c1cncc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
2551 794 None 23 Human Functional pIC50 = 7.3 7.3 -4 13
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
2551.0 794 None 23 Human Functional pIC50 = 7.3 7.3 -4 13
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 794 None 23 Human Functional pIC50 = 7.3 7.3 -4 13
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 794 None 23 Human Functional pIC50 = 7.3 7.3 -4 13
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 794 None 23 Human Functional pIC50 = 7.3 7.3 -4 13
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 794 None 23 Human Functional pIC50 = 7.3 7.3 -4 13
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
137635323 156146 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 444 5 0 6 4.1 COc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4063633 156146 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 444 5 0 6 4.1 COc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
137659754 159260 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 458 4 0 7 3.8 O=C(C1CCN(c2cc(Oc3ccc4c(c3)OCO4)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4099192 159260 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 458 4 0 7 3.8 O=C(C1CCN(c2cc(Oc3ccc4c(c3)OCO4)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
168272462 190164 None 0 Human Functional pIC50 = 7.3 7.3 51 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 428 6 1 5 4.4 Fc1ccc(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5173887 190164 None 0 Human Functional pIC50 = 7.3 7.3 51 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 428 6 1 5 4.4 Fc1ccc(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137659754 159260 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 458 4 0 7 3.8 O=C(C1CCN(c2cc(Oc3ccc4c(c3)OCO4)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4099192 159260 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 458 4 0 7 3.8 O=C(C1CCN(c2cc(Oc3ccc4c(c3)OCO4)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
2066745 95252 None 8 Rat Functional pIC50 = 5.3 5.3 -10 2
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 337 7 1 3 4.0 CCCCCC(=O)Nc1ccc(N2CCN(CC)CC2)c(Cl)c1 10.1016/j.bmcl.2007.12.051
CHEMBL256202 95252 None 8 Rat Functional pIC50 = 5.3 5.3 -10 2
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 337 7 1 3 4.0 CCCCCC(=O)Nc1ccc(N2CCN(CC)CC2)c(Cl)c1 10.1016/j.bmcl.2007.12.051
71718588 86561 None 0 Rat Functional pIC50 = 5.3 5.3 -1 2
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 422 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)C(F)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL2315675 86561 None 0 Rat Functional pIC50 = 5.3 5.3 -1 2
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 422 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)C(F)C2)CC1 10.1016/j.bmcl.2012.10.132
168272462 190164 None 0 Human Functional pIC50 = 7.3 7.3 51 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 428 6 1 5 4.4 Fc1ccc(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5173887 190164 None 0 Human Functional pIC50 = 7.3 7.3 51 2
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 428 6 1 5 4.4 Fc1ccc(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137637971 155879 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 469 4 0 6 3.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3C(F)(F)F)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4060443 155879 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 469 4 0 6 3.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3C(F)(F)F)CC2)nn1 10.1016/j.bmcl.2017.05.042
71718588 86561 None 0 Rat Functional pIC50 = 5.3 5.3 -1 2
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 422 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)C(F)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL2315675 86561 None 0 Rat Functional pIC50 = 5.3 5.3 -1 2
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 422 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)C(F)C2)CC1 10.1016/j.bmcl.2012.10.132
137637971 155879 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 469 4 0 6 3.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3C(F)(F)F)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4060443 155879 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 469 4 0 6 3.4 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3C(F)(F)F)CC2)nn1 10.1016/j.bmcl.2017.05.042
49671356 157425 None 10 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4078704 157425 None 10 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
137408797 190448 None 0 Rat Functional pIC50 = 6.3 6.3 -18 2
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5178468 190448 None 0 Rat Functional pIC50 = 6.3 6.3 -18 2
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
168292831 192096 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1cccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5203077 192096 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1cccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
49671356 157425 None 10 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4078704 157425 None 10 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
137408797 190448 None 0 Rat Functional pIC50 = 6.3 6.3 -18 2
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5178468 190448 None 0 Rat Functional pIC50 = 6.3 6.3 -18 2
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
121053081 155995 None 1 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4061815 155995 None 1 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
168292831 192096 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1cccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5203077 192096 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1cccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
121053081 155995 None 1 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4061815 155995 None 1 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 421 4 0 6 2.6 O=S(=O)(c1ccccc1Cl)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
137654353 159016 None 0 Rat Functional pIC50 = 6.3 6.3 -1 6
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor 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 159016 None 0 Rat Functional pIC50 = 6.3 6.3 -1 6
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor 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
49663949 158031 None 10 Rat Functional pIC50 = 6.3 6.3 -1 2
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4085711 158031 None 10 Rat Functional pIC50 = 6.3 6.3 -1 2
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
137640923 157075 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)C2 10.1016/j.bmcl.2017.04.009
CHEMBL4074229 157075 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)C2 10.1016/j.bmcl.2017.04.009
52176746 157811 None 1 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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
CHEMBL4083307 157811 None 1 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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
137640923 157075 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)C2 10.1016/j.bmcl.2017.04.009
CHEMBL4074229 157075 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 480 5 0 6 4.4 COc1ccc2c(c1)CCN(C(=O)C1CCN(c3cc(Oc4ccc(F)cc4F)ncn3)CC1)C2 10.1016/j.bmcl.2017.04.009
49663949 158031 None 10 Rat Functional pIC50 = 6.2 6.2 -1 2
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
CHEMBL4085711 158031 None 10 Rat Functional pIC50 = 6.2 6.2 -1 2
Antagonist activity at rat M4 receptor by calcium mobilization assayAntagonist activity at rat M4 receptor by calcium mobilization assay
ChEMBL 442 5 0 5 4.6 CCc1ccc(Oc2cc(N3CCC(C(=O)N4CCc5ccccc5C4)CC3)ncn2)cc1 10.1016/j.bmcl.2017.04.009
52176746 157811 None 1 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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
CHEMBL4083307 157811 None 1 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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
49663929 155988 None 13 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 414 4 0 5 4.1 O=C(C1CCN(c2cc(Oc3ccccc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4061637 155988 None 13 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 414 4 0 5 4.1 O=C(C1CCN(c2cc(Oc3ccccc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
16094793 83322 None 0 Human Functional pIC50 = 5.2 5.2 -12 2
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
CHEMBL219118 83322 None 0 Human Functional pIC50 = 5.2 5.2 -12 2
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
49663929 155988 None 13 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 414 4 0 5 4.1 O=C(C1CCN(c2cc(Oc3ccccc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4061637 155988 None 13 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 414 4 0 5 4.1 O=C(C1CCN(c2cc(Oc3ccccc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
137636004 156119 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4063271 156119 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
952858 97728 None 4 Rat Functional pIC50 = 4.2 4.2 -20 3
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 343 4 1 3 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL271519 97728 None 4 Rat Functional pIC50 = 4.2 4.2 -20 3
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 343 4 1 3 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
25070582 61454 None 28 Human Functional pIC50 = 5.2 5.2 -134 9
Antagonist activity at human muscarinic M4 receptorAntagonist activity at human muscarinic M4 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61454 None 28 Human Functional pIC50 = 5.2 5.2 -134 9
Antagonist activity at human muscarinic M4 receptorAntagonist activity at human muscarinic M4 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
137639344 156906 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 5.2 O=C(C1CCN(c2cc(Oc3ccc4ccccc4c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4072231 156906 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 5.2 O=C(C1CCN(c2cc(Oc3ccc4ccccc4c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
156493614 185400 None 0 Human Functional pIC50 = 8.1 8.1 338 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4860985 185400 None 0 Human Functional pIC50 = 8.1 8.1 338 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
164621386 185715 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 447 5 1 6 3.3 CN1Cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2C1=O 10.1021/acsmedchemlett.1c00363
CHEMBL4865665 185715 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 447 5 1 6 3.3 CN1Cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2C1=O 10.1021/acsmedchemlett.1c00363
156493614 185400 None 0 Human Functional pIC50 = 8.1 8.1 338 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4860985 185400 None 0 Human Functional pIC50 = 8.1 8.1 338 2
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
164621386 185715 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 447 5 1 6 3.3 CN1Cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2C1=O 10.1021/acsmedchemlett.1c00363
CHEMBL4865665 185715 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 447 5 1 6 3.3 CN1Cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2C1=O 10.1021/acsmedchemlett.1c00363
137408738 191230 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5189893 191230 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
1726 2497 None 13 Rat Functional pIC50 = 6.2 6.2 -87 8
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 2497 None 13 Rat Functional pIC50 = 6.2 6.2 -87 8
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993.0 2497 None 13 Rat Functional pIC50 = 6.2 6.2 -87 8
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 2497 None 13 Rat Functional pIC50 = 6.2 6.2 -87 8
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 2497 None 13 Rat Functional pIC50 = 6.2 6.2 -87 8
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 2497 None 13 Rat Functional pIC50 = 6.2 6.2 -87 8
Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
137642171 158498 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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)c3cccc(Cl)c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4091095 158498 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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)c3cccc(Cl)c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137408738 191230 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5189893 191230 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
137639344 156906 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 5.2 O=C(C1CCN(c2cc(Oc3ccc4ccccc4c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4072231 156906 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 464 4 0 5 5.2 O=C(C1CCN(c2cc(Oc3ccc4ccccc4c3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
168296286 192373 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccccc1-c1ccc(NC[C@@H]2CC23CCN(CC2CCOCC2)CC3)nn1 10.1016/j.bmcl.2021.128479
CHEMBL5207446 192373 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccccc1-c1ccc(NC[C@@H]2CC23CCN(CC2CCOCC2)CC3)nn1 10.1016/j.bmcl.2021.128479
168296286 192373 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccccc1-c1ccc(NC[C@@H]2CC23CCN(CC2CCOCC2)CC3)nn1 10.1016/j.bmcl.2021.128479
CHEMBL5207446 192373 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 410 6 1 5 4.2 Fc1ccccc1-c1ccc(NC[C@@H]2CC23CCN(CC2CCOCC2)CC3)nn1 10.1016/j.bmcl.2021.128479
142562194 191658 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 458 6 1 5 5.3 Fc1ccc(Cl)c(-c2ccc(NCC3CC4(CCN(CC5CCOCC5)CC4)C3)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5196196 191658 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 458 6 1 5 5.3 Fc1ccc(Cl)c(-c2ccc(NCC3CC4(CCN(CC5CCOCC5)CC4)C3)nn2)c1 10.1016/j.bmcl.2021.128479
137636004 156119 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4063271 156119 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 431 4 0 8 1.7 O=S(=O)(c1ccc2c(c1)OCO2)N1CCN(c2ccc(N3CCCCC3)nn2)CC1 10.1016/j.bmcl.2017.05.042
142562194 191658 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 458 6 1 5 5.3 Fc1ccc(Cl)c(-c2ccc(NCC3CC4(CCN(CC5CCOCC5)CC4)C3)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5196196 191658 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 458 6 1 5 5.3 Fc1ccc(Cl)c(-c2ccc(NCC3CC4(CCN(CC5CCOCC5)CC4)C3)nn2)c1 10.1016/j.bmcl.2021.128479
10092649 193073 None 56 Human Functional pIC50 = 6.1 6.1 -9 11
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M4 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 193073 None 56 Human Functional pIC50 = 6.1 6.1 -9 11
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M4 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 193073 None 56 Human Functional pIC50 = 6.1 6.1 -9 11
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M4 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 193073 None 56 Human Functional pIC50 = 6.1 6.1 -9 11
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M4 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
137642171 158498 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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)c3cccc(Cl)c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4091095 158498 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 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)c3cccc(Cl)c3)CC2)nn1 10.1016/j.bmcl.2017.05.042
137642731 158217 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cc(F)ccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4088103 158217 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cc(F)ccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
2067745 97544 None 4 Rat Functional pIC50 = 5.1 5.1 -13 2
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 415 8 1 4 4.9 CCCCOc1cccc(C(=O)Nc2ccc(N3CCN(CC)CC3)c(Cl)c2)c1 10.1016/j.bmcl.2007.12.051
CHEMBL270580 97544 None 4 Rat Functional pIC50 = 5.1 5.1 -13 2
Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M4 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 415 8 1 4 4.9 CCCCOc1cccc(C(=O)Nc2ccc(N3CCN(CC)CC3)c(Cl)c2)c1 10.1016/j.bmcl.2007.12.051
16094791 83257 None 0 Human Functional pIC50 = 5.1 5.1 -10 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL218755 83257 None 0 Human Functional pIC50 = 5.1 5.1 -10 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
16094783 136567 None 0 Human Functional pIC50 = 5.1 5.1 -100 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL373888 136567 None 0 Human Functional pIC50 = 5.1 5.1 -100 3
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
137642731 158217 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cc(F)ccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4088103 158217 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M4 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3cc(F)ccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
152072967 192238 None 0 Rat Functional pIC50 = 7.1 7.1 -6 2
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5205163 192238 None 0 Rat Functional pIC50 = 7.1 7.1 -6 2
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
152072967 192238 None 0 Rat Functional pIC50 = 7.1 7.1 -6 2
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5205163 192238 None 0 Rat Functional pIC50 = 7.1 7.1 -6 2
Inhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of rat muscarinic acetylcholine M4 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 442 6 1 4 6.0 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCCCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
137653550 158814 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4094472 158814 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
156015153 178307 None 0 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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 178307 None 0 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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 178307 None 0 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M4 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF 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
137653550 158814 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4094472 158814 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 420 4 0 8 2.0 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC[C@@H]3C)nn2)CC1 10.1016/j.bmcl.2017.05.042
137647679 157747 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 449 4 0 6 3.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccccc4Cl)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
CHEMBL4082397 157747 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 449 4 0 6 3.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccccc4Cl)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
137647679 157747 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 449 4 0 6 3.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccccc4Cl)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
CHEMBL4082397 157747 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 449 4 0 6 3.3 CC1(C)CCCN(c2ccc(N3CCN(S(=O)(=O)c4ccccc4Cl)CC3)nn2)C1 10.1016/j.bmcl.2017.05.042
324 1925 None 15 Mouse Functional pKd = 8.0 8.0 - 5
Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4
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(00)80534-X
6436265 1925 None 15 Mouse Functional pKd = 8.0 8.0 - 5
Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4
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(00)80534-X
CHEMBL277642 1925 None 15 Mouse Functional pKd = 8.0 8.0 - 5
Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4
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(00)80534-X
324 1925 None 15 Rat Functional pKd = 8.3 8.3 - 5
Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4
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(00)80534-X
6436265 1925 None 15 Rat Functional pKd = 8.3 8.3 - 5
Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4
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(00)80534-X
CHEMBL277642 1925 None 15 Rat Functional pKd = 8.3 8.3 - 5
Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4
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(00)80534-X
23724781.0 2835 None 19 Human Functional pKd = 8.2 8.2 -4 8
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
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 2835 None 19 Human Functional pKd = 8.2 8.2 -4 8
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
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 2835 None 19 Human Functional pKd = 8.2 8.2 -4 8
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
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 2835 None 19 Human Functional pKd = 8.2 8.2 -4 8
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
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
CHEMBL1354199 2835 None 19 Human Functional pKd = 8.2 8.2 -4 8
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
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 2835 None 19 Human Functional pKd = 8.2 8.2 -4 8
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
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 2835 None 19 Human Functional pKd = 8.2 8.2 -4 8
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
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 2835 None 19 Human Functional pKd = 8.2 8.2 -4 8
Antagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung stripsAntagonist activity at putative muscarinic receptor M4 assessed as contraction of electrically-stimulated guinea pig lung strips
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
1979 77326 None 70 Human Functional pEC50 = 8.3 8.3 1 7
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 77326 None 70 Human Functional pEC50 = 8.3 8.3 1 7
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
123603 883 None 29 Human Functional pEC50 = 8.2 8.2 1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
2684 883 None 29 Human Functional pEC50 = 8.2 8.2 1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
2684.0 883 None 29 Human Functional pEC50 = 8.2 8.2 1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
584 883 None 29 Human Functional pEC50 = 8.2 8.2 1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
9658 883 None 29 Human Functional pEC50 = 8.2 8.2 1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
CHEMBL168815 883 None 29 Human Functional pEC50 = 8.2 8.2 1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
DB00185 883 None 29 Human Functional pEC50 = 8.2 8.2 1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
2166 3123 None 49 Human Functional pEC50 = 8.2 8.2 -2 10
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 3123 None 49 Human Functional pEC50 = 8.2 8.2 -2 10
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 3123 None 49 Human Functional pEC50 = 8.2 8.2 -2 10
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
5910.0 3123 None 49 Human Functional pEC50 = 8.2 8.2 -2 10
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 3123 None 49 Human Functional pEC50 = 8.2 8.2 -2 10
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 3123 None 49 Human Functional pEC50 = 8.2 8.2 -2 10
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
135398737 958 None 93 Human Functional pEC50 = 8.1 8.1 -8 43
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 None 93 Human Functional pEC50 = 8.1 8.1 -8 43
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 None 93 Human Functional pEC50 = 8.1 8.1 -8 43
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 None 93 Human Functional pEC50 = 8.1 8.1 -8 43
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 None 93 Human Functional pEC50 = 8.1 8.1 -8 43
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 None 93 Human Functional pEC50 = 8.1 8.1 -8 43
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5831 215963 None 0 Human Functional pEC50 = 8.1 8.1 1 5
NoneNone
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
5831.0 215963 None 0 Human Functional pEC50 = 8.1 8.1 1 5
NoneNone
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
CHEMBL965 215963 None 0 Human Functional pEC50 = 8.1 8.1 1 5
NoneNone
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
DB00411 215963 None 0 Human Functional pEC50 = 8.1 8.1 1 5
NoneNone
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
306 3456 None 21 Human Functional pEC50 = 8.1 8.1 1 5
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
3536 3456 None 21 Human Functional pEC50 = 8.1 8.1 1 5
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
53930639 3456 None 21 Human Functional pEC50 = 8.1 8.1 1 5
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
9577995 3456 None 21 Human Functional pEC50 = 8.1 8.1 1 5
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
CHEMBL134641 3456 None 21 Human Functional pEC50 = 8.1 8.1 1 5
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
13626 1555 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.
Guide to Pharmacology 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 38888621
140830653 1555 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.
Guide to Pharmacology 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 38888621
140830653.0 1555 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.
Guide to Pharmacology 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 38888621
CHEMBL5314557 1555 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.
Guide to Pharmacology 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 38888621
DB18706 1555 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.Determined in human M<sub>4</sub> HEK293 cell assay using EC<sub>20</sub> of acetylcholine.
Guide to Pharmacology 390 3 0 4 3.5 CC1=CC(=NC2=C1CN(C2)C(=O)CC3CN(C3)C4=CC(=NC=C4)C(F)(F)F)C 38888621
12301 4047 None 30 Human Functional pEC50 = 6.2 6.2 -7 2
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
73774630 4047 None 30 Human Functional pEC50 = 6.2 6.2 -7 2
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
CHEMBL3915634 4047 None 30 Human Functional pEC50 = 6.2 6.2 -7 2
Potentiation of ACh response at human receptorPotentiation of ACh response at human receptor
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
1541501 4024 None 29 Rat Functional pEC50 = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 18772318
3256 4024 None 29 Rat Functional pEC50 = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 18772318
CHEMBL4461667 4024 None 29 Rat Functional pEC50 = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 18772318
3263 4025 None 58 Rat Functional pEC50 = 6.4 6.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 18772318
864492 4025 None 58 Rat Functional pEC50 = 6.4 6.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 18772318
CHEMBL1978713 4025 None 58 Rat Functional pEC50 = 6.4 6.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 18772318
12301 4047 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
UnclassifiedUnclassified
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
73774630 4047 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
UnclassifiedUnclassified
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
CHEMBL3915634 4047 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
UnclassifiedUnclassified
Guide to Pharmacology 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 25137629
288 252 None 0 Human Functional pEC50 None 4.8 4.8 -7 5
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
6979053 252 None 0 Human Functional pEC50 None 4.8 4.8 -7 5
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
286 251 None 0 Human Functional pEC50 None 5.4 5.4 -7 5
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
6954180 251 None 0 Human Functional pEC50 None 5.4 5.4 -7 5
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
11536903 2397 None 68 Human Functional pKB = 5.2 5.2 -28 2
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 14595031
11536903 2397 None 68 Human Functional pKB = 5.2 5.2 -28 2
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 18678919
3262 2397 None 68 Human Functional pKB = 5.2 5.2 -28 2
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 14595031
3262 2397 None 68 Human Functional pKB = 5.2 5.2 -28 2
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 18678919
CHEMBL3770346 2397 None 68 Human Functional pKB = 5.2 5.2 -28 2
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 14595031
CHEMBL3770346 2397 None 68 Human Functional pKB = 5.2 5.2 -28 2
UnclassifiedUnclassified
Guide to Pharmacology 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 18678919


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
367 3824 None 12 Human Binding pAC50 = 9.5 9.5 -10 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
5487427 3824 None 12 Human Binding pAC50 = 9.5 9.5 -10 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
5487427.0 3824 None 12 Human Binding pAC50 = 9.5 9.5 -10 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
8592 3824 None 12 Human Binding pAC50 = 9.5 9.5 -10 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
CHEMBL1900528 3824 None 12 Human Binding pAC50 = 9.5 9.5 -10 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
CHEMBL3305968 3824 None 12 Human Binding pAC50 = 9.5 9.5 -10 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
CHEMBL4650755 3824 None 12 Human Binding pAC50 = 9.5 9.5 -10 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
DB01409 3824 None 12 Human Binding pAC50 = 9.5 9.5 -10 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
11693 1827 None 16 Human Binding pAC50 = 9 9.0 1 5
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494 1827 None 16 Human Binding pAC50 = 9 9.0 1 5
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494.0 1827 None 16 Human Binding pAC50 = 9 9.0 1 5
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
4302 1827 None 16 Human Binding pAC50 = 9 9.0 1 5
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
7459 1827 None 16 Human Binding pAC50 = 9 9.0 1 5
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
9933193.0 1827 None 16 Human Binding pAC50 = 9 9.0 1 5
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
CHEMBL1201335 1827 None 16 Human Binding pAC50 = 9 9.0 1 5
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
DB00986 1827 None 16 Human Binding pAC50 = 9 9.0 1 5
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
25897919 55652 None 14 Human Binding pAC50 = 8.9 8.9 -3 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
657308.0 55652 None 14 Human Binding pAC50 = 8.9 8.9 -3 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
657309 55652 None 14 Human Binding pAC50 = 8.9 8.9 -3 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
CHEMBL1464005 55652 None 14 Human Binding pAC50 = 8.9 8.9 -3 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
CHEMBL1621597 55652 None 14 Human Binding pAC50 = 8.9 8.9 -3 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
DB00332 55652 None 14 Human Binding pAC50 = 8.9 8.9 -3 8
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
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 10.1038/s41467-023-40064-9
1427 2013 None 54 Human Binding pAC50 = 6.0 6.0 -2 27
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2013 None 54 Human Binding pAC50 = 6.0 6.0 -2 27
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2013 None 54 Human Binding pAC50 = 6.0 6.0 -2 27
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2013 None 54 Human Binding pAC50 = 6.0 6.0 -2 27
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2013 None 54 Human Binding pAC50 = 6.0 6.0 -2 27
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3180 14473 None 41 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201217 14473 None 41 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
2284 3182 None 33 Human Binding pAC50 = 5.8 5.8 -7 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3182 None 33 Human Binding pAC50 = 5.8 5.8 -7 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3182 None 33 Human Binding pAC50 = 5.8 5.8 -7 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3182 None 33 Human Binding pAC50 = 5.8 5.8 -7 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3182 None 33 Human Binding pAC50 = 5.8 5.8 -7 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
135398745 2914 None 112 Human Binding pAC50 = 6.5 6.5 -32 65
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
135398745.0 2914 None 112 Human Binding pAC50 = 6.5 6.5 -32 65
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2914 None 112 Human Binding pAC50 = 6.5 6.5 -32 65
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2914 None 112 Human Binding pAC50 = 6.5 6.5 -32 65
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2914 None 112 Human Binding pAC50 = 6.5 6.5 -32 65
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
1224 1432 None 83 Human Binding pAC50 = 5.5 5.5 -3 13
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 1432 None 83 Human Binding pAC50 = 5.5 5.5 -3 13
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100.0 1432 None 83 Human Binding pAC50 = 5.5 5.5 -3 13
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 1432 None 83 Human Binding pAC50 = 5.5 5.5 -3 13
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 1432 None 83 Human Binding pAC50 = 5.5 5.5 -3 13
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 1432 None 83 Human Binding pAC50 = 5.5 5.5 -3 13
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 1432 None 83 Human Binding pAC50 = 5.5 5.5 -3 13
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
43815 186920 None 64 Human Binding pAC50 = 5.5 5.5 -8 25
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL1708 186920 None 64 Human Binding pAC50 = 5.5 5.5 -8 25
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 186920 None 64 Human Binding pAC50 = 5.5 5.5 -8 25
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
1613 2348 None 53 Human Binding pAC50 = 5.4 5.4 -43 44
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 None 53 Human Binding pAC50 = 5.4 5.4 -43 44
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 None 53 Human Binding pAC50 = 5.4 5.4 -43 44
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964.0 2348 None 53 Human Binding pAC50 = 5.4 5.4 -43 44
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 None 53 Human Binding pAC50 = 5.4 5.4 -43 44
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 None 53 Human Binding pAC50 = 5.4 5.4 -43 44
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2784 952 None 13 Human Binding pAC50 = 8.3 8.3 - 3
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
2784.0 952 None 13 Human Binding pAC50 = 8.3 8.3 - 3
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
351 952 None 13 Human Binding pAC50 = 8.3 8.3 - 3
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
366 952 None 13 Human Binding pAC50 = 8.3 8.3 - 3
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
676 952 None 13 Human Binding pAC50 = 8.3 8.3 - 3
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL620 952 None 13 Human Binding pAC50 = 8.3 8.3 - 3
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
DB00771 952 None 13 Human Binding pAC50 = 8.3 8.3 - 3
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
3158 56267 None 27 Human Binding pAC50 = 6.3 6.3 -40 20
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3158.0 56267 None 27 Human Binding pAC50 = 6.3 6.3 -40 20
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56267 None 27 Human Binding pAC50 = 6.3 6.3 -40 20
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56267 None 27 Human Binding pAC50 = 6.3 6.3 -40 20
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
1971 2866 None 38 Human Binding pAC50 = 6.2 6.2 -3 30
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2866 None 38 Human Binding pAC50 = 6.2 6.2 -3 30
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2866 None 38 Human Binding pAC50 = 6.2 6.2 -3 30
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543.0 2866 None 38 Human Binding pAC50 = 6.2 6.2 -3 30
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2866 None 38 Human Binding pAC50 = 6.2 6.2 -3 30
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2866 None 38 Human Binding pAC50 = 6.2 6.2 -3 30
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
191 403 None 98 Human Binding pAC50 = 5.1 5.1 -29 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 None 98 Human Binding pAC50 = 5.1 5.1 -29 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 None 98 Human Binding pAC50 = 5.1 5.1 -29 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170.0 403 None 98 Human Binding pAC50 = 5.1 5.1 -29 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 None 98 Human Binding pAC50 = 5.1 5.1 -29 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 None 98 Human Binding pAC50 = 5.1 5.1 -29 29
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
72713421 102536 None 0 Human Binding pEC50 = 7 7.0 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1F 10.1021/jm401032k
CHEMBL2435361 102536 None 0 Human Binding pEC50 = 7 7.0 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1F 10.1021/jm401032k
CHEMBL3040619 102536 None 0 Human Binding pEC50 = 7 7.0 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1F 10.1021/jm401032k
CHEMBL5288291 194415 None 0 Human Binding pEC50 = 7 7.0 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
CHEMBL5288291 194415 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
44176134 102535 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL2435357 102535 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040618 102535 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
44176134 102535 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL2435357 102535 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040618 102535 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
156016090 177684 None 0 Rat Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 404 3 2 6 2.5 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4641848 177684 None 0 Rat Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 404 3 2 6 2.5 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
44176127 102522 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
CHEMBL2435354 102522 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040499 102522 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
3263 4025 None 58 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
864492 4025 None 58 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
CHEMBL1978713 4025 None 58 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
89777266 147908 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1021/acsmedchemlett.6b00461
CHEMBL3933538 147908 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1021/acsmedchemlett.6b00461
156013904 177239 None 0 Rat Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 395 3 2 7 2.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4635732 177239 None 0 Rat Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 395 3 2 7 2.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
2230 465 None 60 Human Binding pEC50 = 6.9 6.9 -218 10
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 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
296 465 None 60 Human Binding pEC50 = 6.9 6.9 -218 10
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 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 465 None 60 Human Binding pEC50 = 6.9 6.9 -218 10
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 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 465 None 60 Human Binding pEC50 = 6.9 6.9 -218 10
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 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
3263 4025 None 58 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
864492 4025 None 58 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
CHEMBL1978713 4025 None 58 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
44176127 102522 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
CHEMBL2435354 102522 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040499 102522 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
44176132 102532 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL2435358 102532 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040593 102532 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
89777266 147908 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1021/acsmedchemlett.6b00461
CHEMBL3933538 147908 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1021/acsmedchemlett.6b00461
44176132 102532 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL2435358 102532 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040593 102532 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL5287096 194613 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5315302 194613 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
187 255 None 39 Human Binding pEC50 = 6.9 6.9 -6 9
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
187.0 255 None 39 Human Binding pEC50 = 6.9 6.9 -6 9
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
294 255 None 39 Human Binding pEC50 = 6.9 6.9 -6 9
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
65 255 None 39 Human Binding pEC50 = 6.9 6.9 -6 9
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
8593 255 None 39 Human Binding pEC50 = 6.9 6.9 -6 9
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
CHEMBL667 255 None 39 Human Binding pEC50 = 6.9 6.9 -6 9
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
DB03128 255 None 39 Human Binding pEC50 = 6.9 6.9 -6 9
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
72713420 102518 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL2435360 102518 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040457 102518 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
72713420 102518 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL2435360 102518 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040457 102518 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL5269733 193607 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 361 4 2 7 2.4 COc1ncc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5269733 193607 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 361 4 2 7 2.4 COc1ncc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
53382542 86313 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 86313 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137640201 156961 None 2 Human Binding pEC50 = 6.8 6.8 -575 13
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156961 None 2 Human Binding pEC50 = 6.8 6.8 -575 13
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
53382542 86313 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 86313 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
91468 207064 None 15 Human Binding pEC50 = 4.8 4.8 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
CHEMBL91776 207064 None 15 Human Binding pEC50 = 4.8 4.8 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
156015762 177544 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 3 1 8 2.9 Cn1nnc2ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL4640254 177544 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 3 1 8 2.9 Cn1nnc2ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc3c21 10.1016/j.bmcl.2019.126811
89777266 147908 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3933538 147908 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
2551 794 None 23 Human Binding pEC50 = 6.8 6.8 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
2551.0 794 None 23 Human Binding pEC50 = 6.8 6.8 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
298 794 None 23 Human Binding pEC50 = 6.8 6.8 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
488 794 None 23 Human Binding pEC50 = 6.8 6.8 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
CHEMBL965 794 None 23 Human Binding pEC50 = 6.8 6.8 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
DB00411 794 None 23 Human Binding pEC50 = 6.8 6.8 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
156020012 178096 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 391 3 2 7 1.9 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4647876 178096 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 391 3 2 7 1.9 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
3652 4097 None 79 Human Binding pEC50 = 7.8 7.8 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 4097 None 79 Human Binding pEC50 = 7.8 7.8 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 4097 None 79 Human Binding pEC50 = 7.8 7.8 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809.0 4097 None 79 Human Binding pEC50 = 7.8 7.8 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 4097 None 79 Human Binding pEC50 = 7.8 7.8 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 4097 None 79 Human Binding pEC50 = 7.8 7.8 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
156013280 177491 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4639387 177491 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)c(N)c21 10.1016/j.bmcl.2019.126811
156016660 177707 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 414 5 2 6 4.1 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4642156 177707 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 414 5 2 6 4.1 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
53382523 76062 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2057417 76062 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382523 76062 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2057417 76062 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
118719922 115775 None 0 Human Binding pEC50 = 7.7 7.7 -1 5
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 115775 None 0 Human Binding pEC50 = 7.7 7.7 -1 5
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
156014219 177247 None 0 Rat Binding pEC50 = 6.7 6.7 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 351 4 1 6 3.6 COc1ccc(CNc2ncnc3c2ccc2nn(C)c(C)c23)cc1F 10.1016/j.bmcl.2019.126811
CHEMBL4635909 177247 None 0 Rat Binding pEC50 = 6.7 6.7 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 351 4 1 6 3.6 COc1ccc(CNc2ncnc3c2ccc2nn(C)c(C)c23)cc1F 10.1016/j.bmcl.2019.126811
3652 4097 None 79 Human Binding pEC50 = 6.7 6.7 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 4097 None 79 Human Binding pEC50 = 6.7 6.7 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 4097 None 79 Human Binding pEC50 = 6.7 6.7 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809.0 4097 None 79 Human Binding pEC50 = 6.7 6.7 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 4097 None 79 Human Binding pEC50 = 6.7 6.7 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 4097 None 79 Human Binding pEC50 = 6.7 6.7 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
118719926 115780 None 0 Human Binding pEC50 = 5.7 5.7 -102 8
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 115780 None 0 Human Binding pEC50 = 5.7 5.7 -102 8
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
16757565 15280 None 0 Human Binding pEC50 = 6.7 6.7 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
CHEMBL1212989 15280 None 0 Human Binding pEC50 = 6.7 6.7 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
CHEMBL2435356 15280 None 0 Human Binding pEC50 = 6.7 6.7 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
16757565 15280 None 0 Human Binding pEC50 = 6.7 6.7 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
CHEMBL1212989 15280 None 0 Human Binding pEC50 = 6.7 6.7 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
CHEMBL2435356 15280 None 0 Human Binding pEC50 = 6.7 6.7 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
2551 794 None 23 Human Binding pEC50 = 5.7 5.7 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
2551.0 794 None 23 Human Binding pEC50 = 5.7 5.7 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
298 794 None 23 Human Binding pEC50 = 5.7 5.7 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
488 794 None 23 Human Binding pEC50 = 5.7 5.7 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
CHEMBL965 794 None 23 Human Binding pEC50 = 5.7 5.7 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
DB00411 794 None 23 Human Binding pEC50 = 5.7 5.7 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
156013839 177174 None 0 Rat Binding pEC50 = 6.7 6.7 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 409 4 1 8 3.2 COc1cc(N2CC(Nc3ncnc4c3ccc3nn(C)c(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4634770 177174 None 0 Rat Binding pEC50 = 6.7 6.7 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 409 4 1 8 3.2 COc1cc(N2CC(Nc3ncnc4c3ccc3nn(C)c(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
2551 794 None 23 Human Binding pEC50 = 5.6 5.6 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
2551.0 794 None 23 Human Binding pEC50 = 5.6 5.6 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
298 794 None 23 Human Binding pEC50 = 5.6 5.6 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
488 794 None 23 Human Binding pEC50 = 5.6 5.6 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
CHEMBL965 794 None 23 Human Binding pEC50 = 5.6 5.6 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
DB00411 794 None 23 Human Binding pEC50 = 5.6 5.6 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
3263 4025 None 58 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
864492 4025 None 58 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
CHEMBL1978713 4025 None 58 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2012.10.073
156018661 177835 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 387 4 2 8 1.2 COc1cc(N2CC(NC(=O)c3ccc4nnn(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4644004 177835 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 387 4 2 8 1.2 COc1cc(N2CC(NC(=O)c3ccc4nnn(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
156022087 178196 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 390 3 1 6 2.7 Cc1nc2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4649459 178196 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 390 3 1 6 2.7 Cc1nc2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL5267403 193528 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 343 4 2 7 2.2 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cn1 10.1021/acsmedchemlett.6b00461
72713423 102524 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 377 4 2 5 3.7 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1F 10.1021/jm401032k
CHEMBL2435362 102524 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 377 4 2 5 3.7 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1F 10.1021/jm401032k
CHEMBL3040500 102524 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 377 4 2 5 3.7 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1F 10.1021/jm401032k
CHEMBL5267403 193528 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 343 4 2 7 2.2 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cn1 10.1021/acsmedchemlett.6b00461
10442081 102608 None 9 Human Binding pEC50 = 6.6 6.6 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL304142 102608 None 9 Human Binding pEC50 = 6.6 6.6 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
72713423 102524 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 377 4 2 5 3.7 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1F 10.1021/jm401032k
CHEMBL2435362 102524 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 377 4 2 5 3.7 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1F 10.1021/jm401032k
CHEMBL3040500 102524 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 377 4 2 5 3.7 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1F 10.1021/jm401032k
45142486 52359 None 0 Rat Binding pEC50 = 5.6 5.6 - 0
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1021/acs.jmedchem.8b00875
CHEMBL1589763 52359 None 0 Rat Binding pEC50 = 5.6 5.6 - 0
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1021/acs.jmedchem.8b00875
156016190 177699 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 413 3 1 7 3.8 Cc1c2c(ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4642055 177699 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 413 3 1 7 3.8 Cc1c2c(ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
45501061 156775 None 12 Rat Binding pEC50 = 5.6 5.6 - 0
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced responsePositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced response
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4070787 156775 None 12 Rat Binding pEC50 = 5.6 5.6 - 0
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced responsePositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced response
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
156010562 177046 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632555 177046 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 389 3 1 5 3.2 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
89777239 163953 None 24 Rat Binding pEC50 = 7.6 7.6 - 0
Positive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 163953 None 24 Rat Binding pEC50 = 7.6 7.6 - 0
Positive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5268842 163953 None 24 Rat Binding pEC50 = 7.6 7.6 - 0
Positive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
89777239 163953 None 24 Rat Binding pEC50 = 7.6 7.6 - 0
Positive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 163953 None 24 Rat Binding pEC50 = 7.6 7.6 - 0
Positive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5268842 163953 None 24 Rat Binding pEC50 = 7.6 7.6 - 0
Positive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5287159 194619 None 0 Human Binding pEC50 = 5.6 5.6 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 560 13 1 4 4.5 CC(C)(CN1C(=O)c2cccc3cccc(c23)C1=O)C[N+](C)(C)CCCCCC[n+]1c[nH]c(CC2COC(=O)C2)c1 10.1021/acs.jnatprod.2c01079
CHEMBL5315392 194619 None 0 Human Binding pEC50 = 5.6 5.6 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 560 13 1 4 4.5 CC(C)(CN1C(=O)c2cccc3cccc(c23)C1=O)C[N+](C)(C)CCCCCC[n+]1c[nH]c(CC2COC(=O)C2)c1 10.1021/acs.jnatprod.2c01079
10236758 115772 None 5 Human Binding pEC50 = 6.6 6.6 -213 13
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 115772 None 5 Human Binding pEC50 = 6.6 6.6 -213 13
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
134263768 183141 None 7 Rat Binding pEC50 = 7.6 7.6 - 0
Positive allosteric modulation of rat M4 receptorPositive allosteric modulation of rat M4 receptor
ChEMBL 439 4 2 9 2.0 COc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4795177 183141 None 7 Rat Binding pEC50 = 7.6 7.6 - 0
Positive allosteric modulation of rat M4 receptorPositive allosteric modulation of rat M4 receptor
ChEMBL 439 4 2 9 2.0 COc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
90005322 171919 None 0 Rat Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 429 4 2 6 3.4 Cc1cncc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4469998 171919 None 0 Rat Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 429 4 2 6 3.4 Cc1cncc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c12 10.1016/j.bmcl.2019.06.032
156014184 177197 None 0 Rat Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cn4c(C)c(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4635170 177197 None 0 Rat Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cn4c(C)c(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
10261985 203949 None 0 Human Binding pEC50 = 7.5 7.5 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69306 203949 None 0 Human Binding pEC50 = 7.5 7.5 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
118719921 115774 None 0 Human Binding pEC50 = 7.5 7.5 -1 5
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 115774 None 0 Human Binding pEC50 = 7.5 7.5 -1 5
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
72713214 102521 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3)sc2n1 10.1021/jm401032k
CHEMBL2435355 102521 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3)sc2n1 10.1021/jm401032k
CHEMBL3040488 102521 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3)sc2n1 10.1021/jm401032k
72713214 102521 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3)sc2n1 10.1021/jm401032k
CHEMBL2435355 102521 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3)sc2n1 10.1021/jm401032k
CHEMBL3040488 102521 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3)sc2n1 10.1021/jm401032k
156012754 177311 None 0 Rat Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 5 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4636845 177311 None 0 Rat Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 5 2 6 3.7 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
302 2977 None 25 Human Binding pEC50 = 7.5 7.5 -7 8
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
4630 2977 None 25 Human Binding pEC50 = 7.5 7.5 -7 8
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
CHEMBL7634 2977 None 25 Human Binding pEC50 = 7.5 7.5 -7 8
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
156014638 177225 None 0 Rat Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 390 3 1 6 2.6 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ncc2nn1C 10.1016/j.bmcl.2019.126812
CHEMBL4635575 177225 None 0 Rat Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 390 3 1 6 2.6 Cc1c2cc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ncc2nn1C 10.1016/j.bmcl.2019.126812
2166 3123 None 49 Human Binding pEC50 = 5.5 5.5 -17 8
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
305 3123 None 49 Human Binding pEC50 = 5.5 5.5 -17 8
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
5910 3123 None 49 Human Binding pEC50 = 5.5 5.5 -17 8
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
5910.0 3123 None 49 Human Binding pEC50 = 5.5 5.5 -17 8
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
CHEMBL550 3123 None 49 Human Binding pEC50 = 5.5 5.5 -17 8
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
DB01085 3123 None 49 Human Binding pEC50 = 5.5 5.5 -17 8
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
156012624 177419 None 0 Rat Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)n(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4638506 177419 None 0 Rat Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)n(C)nc4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
72713422 102529 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1 10.1021/jm401032k
CHEMBL2434973 102529 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1 10.1021/jm401032k
CHEMBL3040554 102529 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1 10.1021/jm401032k
118719922 115775 None 0 Human Binding pEC50 = 7.5 7.5 -1 5
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 115775 None 0 Human Binding pEC50 = 7.5 7.5 -1 5
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
72713422 102529 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1 10.1021/jm401032k
CHEMBL2434973 102529 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1 10.1021/jm401032k
CHEMBL3040554 102529 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c(F)c1 10.1021/jm401032k
CHEMBL5270076 194606 None 0 Human Binding pEC50 = 4.4 4.4 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 574 13 0 5 4.5 Cn1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cc1CC1COC(=O)C1 10.1021/acs.jnatprod.2c01079
CHEMBL5315256 194606 None 0 Human Binding pEC50 = 4.4 4.4 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 574 13 0 5 4.5 Cn1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cc1CC1COC(=O)C1 10.1021/acs.jnatprod.2c01079
156011257 177328 None 0 Rat Binding pEC50 = 6.4 6.4 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 443 3 1 5 3.9 Cn1c(C(F)(F)F)nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
CHEMBL4637175 177328 None 0 Rat Binding pEC50 = 6.4 6.4 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 443 3 1 5 3.9 Cn1c(C(F)(F)F)nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126812
1541501 4024 None 29 Rat Binding pEC50 = 6.4 6.4 - 0
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.8b00875
3256 4024 None 29 Rat Binding pEC50 = 6.4 6.4 - 0
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.8b00875
CHEMBL4461667 4024 None 29 Rat Binding pEC50 = 6.4 6.4 - 0
Positive allosteric modulation of rat M4 AchRPositive allosteric modulation of rat M4 AchR
ChEMBL 355 3 2 6 3.2 Cc1cc(C)c2c(n1)sc(c2N)C(=O)NCc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.8b00875
CHEMBL5276239 193891 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5276239 193891 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1cc(F)c(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
156011081 177069 None 0 Rat Binding pEC50 = 7.4 7.4 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 404 3 2 6 2.8 Cc1c2c(N)c(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632962 177069 None 0 Rat Binding pEC50 = 7.4 7.4 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 404 3 2 6 2.8 Cc1c2c(N)c(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL5269998 193614 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1F 10.1021/acsmedchemlett.6b00461
CHEMBL5269998 193614 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1F 10.1021/acsmedchemlett.6b00461
156014224 177257 None 0 Rat Binding pEC50 = 6.4 6.4 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 389 3 1 5 3.3 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4636061 177257 None 0 Rat Binding pEC50 = 6.4 6.4 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 389 3 1 5 3.3 Cc1nc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
137647620 157598 None 0 Rat Binding pEC50 = 6.4 6.4 - 0
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced responsePositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced response
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4080878 157598 None 0 Rat Binding pEC50 = 6.4 6.4 - 0
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced responsePositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced response
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
2551 794 None 23 Human Binding pEC50 = 7.4 7.4 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
2551.0 794 None 23 Human Binding pEC50 = 7.4 7.4 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
298 794 None 23 Human Binding pEC50 = 7.4 7.4 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
488 794 None 23 Human Binding pEC50 = 7.4 7.4 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
CHEMBL965 794 None 23 Human Binding pEC50 = 7.4 7.4 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
DB00411 794 None 23 Human Binding pEC50 = 7.4 7.4 -21 11
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
CHEMBL5265850 193458 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 374 4 2 6 3.5 COc1ccc([C@H](C)NC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5265850 193458 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 374 4 2 6 3.5 COc1ccc([C@H](C)NC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
3263 4025 None 58 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2016.11.086
864492 4025 None 58 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2016.11.086
CHEMBL1978713 4025 None 58 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1016/j.bmcl.2016.11.086
CHEMBL5285668 194630 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5315497 194630 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
89777239 163953 None 24 Human Binding pEC50 = 7.3 7.3 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 163953 None 24 Human Binding pEC50 = 7.3 7.3 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5268842 163953 None 24 Human Binding pEC50 = 7.3 7.3 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
89777239 163953 None 24 Human Binding pEC50 = 7.3 7.3 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 163953 None 24 Human Binding pEC50 = 7.3 7.3 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5268842 163953 None 24 Human Binding pEC50 = 7.3 7.3 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
72713209 102534 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1cccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c1 10.1021/jm401032k
CHEMBL2435349 102534 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1cccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c1 10.1021/jm401032k
CHEMBL3040603 102534 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1cccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c1 10.1021/jm401032k
72713209 102534 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1cccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c1 10.1021/jm401032k
CHEMBL2435349 102534 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1cccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c1 10.1021/jm401032k
CHEMBL3040603 102534 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1cccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)c1 10.1021/jm401032k
72713419 102528 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)c(F)cc3F)sc2n1 10.1021/jm401032k
CHEMBL2435359 102528 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)c(F)cc3F)sc2n1 10.1021/jm401032k
CHEMBL3040531 102528 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)c(F)cc3F)sc2n1 10.1021/jm401032k
72713419 102528 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)c(F)cc3F)sc2n1 10.1021/jm401032k
CHEMBL2435359 102528 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)c(F)cc3F)sc2n1 10.1021/jm401032k
CHEMBL3040531 102528 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)c(F)cc3F)sc2n1 10.1021/jm401032k
14925759 158038 None 6 Human Binding pEC50 = 6.2 6.2 -3235 13
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 158038 None 6 Human Binding pEC50 = 6.2 6.2 -3235 13
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL5282936 194176 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 346 3 3 6 2.7 Cc1nnc2sc(C(=O)NCc3ccc(O)c(F)c3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
CHEMBL5282936 194176 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 346 3 3 6 2.7 Cc1nnc2sc(C(=O)NCc3ccc(O)c(F)c3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
3652 4097 None 79 Human Binding pEC50 = 5.2 5.2 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 4097 None 79 Human Binding pEC50 = 5.2 5.2 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 4097 None 79 Human Binding pEC50 = 5.2 5.2 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809.0 4097 None 79 Human Binding pEC50 = 5.2 5.2 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 4097 None 79 Human Binding pEC50 = 5.2 5.2 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 4097 None 79 Human Binding pEC50 = 5.2 5.2 -3 18
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
2551 794 None 23 Human Binding pEC50 = 5.2 5.2 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
2551.0 794 None 23 Human Binding pEC50 = 5.2 5.2 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
298 794 None 23 Human Binding pEC50 = 5.2 5.2 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
488 794 None 23 Human Binding pEC50 = 5.2 5.2 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
CHEMBL965 794 None 23 Human Binding pEC50 = 5.2 5.2 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
DB00411 794 None 23 Human Binding pEC50 = 5.2 5.2 -21 11
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
101882890 115776 None 0 Human Binding pEC50 = 4.2 4.2 -1 5
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354069 115776 None 0 Human Binding pEC50 = 4.2 4.2 -1 5
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
10442337 203948 None 2 Human Binding pEC50 = 7.2 7.2 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69305 203948 None 2 Human Binding pEC50 = 7.2 7.2 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
118719921 115774 None 0 Human Binding pEC50 = 5.2 5.2 -1 5
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 115774 None 0 Human Binding pEC50 = 5.2 5.2 -1 5
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
156011921 177399 None 0 Rat Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 388 3 2 6 2.3 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4638291 177399 None 0 Rat Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 388 3 2 6 2.3 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
156010821 177064 None 0 Rat Binding pEC50 = 6.1 6.1 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126811
CHEMBL4632855 177064 None 0 Rat Binding pEC50 = 6.1 6.1 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 376 3 1 6 2.3 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc21 10.1016/j.bmcl.2019.126811
CHEMBL5272950 193740 None 0 Human Binding pEC50 = 5.1 5.1 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 166 2 1 3 0.5 O=C1C[C@@H](Cc2cnc[nH]2)CO1 10.1021/acs.jnatprod.2c01079
2551 794 None 23 Human Binding pEC50 = 7.1 7.1 -21 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 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
2551.0 794 None 23 Human Binding pEC50 = 7.1 7.1 -21 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 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
298 794 None 23 Human Binding pEC50 = 7.1 7.1 -21 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 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
488 794 None 23 Human Binding pEC50 = 7.1 7.1 -21 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 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 794 None 23 Human Binding pEC50 = 7.1 7.1 -21 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 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 794 None 23 Human Binding pEC50 = 7.1 7.1 -21 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 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
89777239 163953 None 24 Human Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 163953 None 24 Human Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5268842 163953 None 24 Human Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
89777239 163953 None 24 Human Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL4207737 163953 None 24 Human Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5268842 163953 None 24 Human Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
156013272 177483 None 0 Rat Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 4 2 7 2.1 COc1cc(N2CC(NC(=O)c3ccc4nn(C)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4639222 177483 None 0 Rat Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 4 2 7 2.1 COc1cc(N2CC(NC(=O)c3ccc4nn(C)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL5285036 194276 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1c(F)cc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5285036 194276 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 378 4 2 6 3.1 COc1c(F)cc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1F 10.1021/acsmedchemlett.6b00461
CHEMBL5272517 193728 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
45142486 52359 None 0 Rat Binding pEC50 = 6.1 6.1 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1016/j.bmcl.2012.10.073
CHEMBL1589763 52359 None 0 Rat Binding pEC50 = 6.1 6.1 - 0
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1016/j.bmcl.2012.10.073
CHEMBL5272517 193728 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 360 4 2 6 3.0 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)c(F)c1 10.1021/acsmedchemlett.6b00461
45142486 52359 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulation of human M4 AchRPositive allosteric modulation of human M4 AchR
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1021/acs.jmedchem.8b00875
CHEMBL1589763 52359 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulation of human M4 AchRPositive allosteric modulation of human M4 AchR
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c12 10.1021/acs.jmedchem.8b00875
CHEMBL5274545 194648 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 630 16 0 5 5.9 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5315812 194648 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 630 16 0 5 5.9 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5265891 193462 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 328 3 3 6 2.5 Cc1nnc2sc(C(=O)NCc3ccc(O)cc3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
CHEMBL5265891 193462 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assayPositive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
ChEMBL 328 3 3 6 2.5 Cc1nnc2sc(C(=O)NCc3ccc(O)cc3)c(N)c2c1C 10.1021/acsmedchemlett.6b00461
367 3824 None 12 Human Binding pIC50 = 10.4 10.4 -10 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 3824 None 12 Human Binding pIC50 = 10.4 10.4 -10 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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
5487427.0 3824 None 12 Human Binding pIC50 = 10.4 10.4 -10 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 3824 None 12 Human Binding pIC50 = 10.4 10.4 -10 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 3824 None 12 Human Binding pIC50 = 10.4 10.4 -10 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 3824 None 12 Human Binding pIC50 = 10.4 10.4 -10 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 3824 None 12 Human Binding pIC50 = 10.4 10.4 -10 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 3824 None 12 Human Binding pIC50 = 10.4 10.4 -10 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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
11693 1827 None 16 Human Binding pIC50 = 9.8 9.8 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 1827 None 16 Human Binding pIC50 = 9.8 9.8 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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
3494.0 1827 None 16 Human Binding pIC50 = 9.8 9.8 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 1827 None 16 Human Binding pIC50 = 9.8 9.8 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 1827 None 16 Human Binding pIC50 = 9.8 9.8 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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
9933193.0 1827 None 16 Human Binding pIC50 = 9.8 9.8 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 1827 None 16 Human Binding pIC50 = 9.8 9.8 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 1827 None 16 Human Binding pIC50 = 9.8 9.8 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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
11434515 261 None 6 Human Binding pIC50 = 9.7 9.7 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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
11434515.0 261 None 6 Human Binding pIC50 = 9.7 9.7 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 261 None 6 Human Binding pIC50 = 9.7 9.7 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 261 None 6 Human Binding pIC50 = 9.7 9.7 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 261 None 6 Human Binding pIC50 = 9.7 9.7 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 261 None 6 Human Binding pIC50 = 9.7 9.7 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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 261 None 6 Human Binding pIC50 = 9.7 9.7 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 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
2551 794 None 23 Human Binding pIC50 = 9.4 9.4 -21 11
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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
2551.0 794 None 23 Human Binding pIC50 = 9.4 9.4 -21 11
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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
298 794 None 23 Human Binding pIC50 = 9.4 9.4 -21 11
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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
488 794 None 23 Human Binding pIC50 = 9.4 9.4 -21 11
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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 794 None 23 Human Binding pIC50 = 9.4 9.4 -21 11
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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 794 None 23 Human Binding pIC50 = 9.4 9.4 -21 11
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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
156493833 184907 None 2 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 7 3.6 Cn1cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2n1 10.1021/acsmedchemlett.1c00363
CHEMBL4853244 184907 None 2 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 7 3.6 Cn1cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2n1 10.1021/acsmedchemlett.1c00363
1734 116 None 10 Human Binding pIC50 = 9.3 9.3 -1 12
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M4 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 None 10 Human Binding pIC50 = 9.3 9.3 -1 12
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M4 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 None 10 Human Binding pIC50 = 9.3 9.3 -1 12
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M4 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 None 10 Human Binding pIC50 = 9.3 9.3 -1 12
Displacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M4 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 None 10 Human Binding pIC50 = 9.3 9.3 -1 12
Displacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M4 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 None 10 Human Binding pIC50 = 9.3 9.3 -1 12
Displacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M4 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
11968014 12758 None 5 Human Binding pIC50 = 9.2 9.2 -12 9
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
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/acs.jmedchem.8b00265
119680147.0 12758 None 5 Human Binding pIC50 = 9.2 9.2 -12 9
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
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/acs.jmedchem.8b00265
CHEMBL1187846 12758 None 5 Human Binding pIC50 = 9.2 9.2 -12 9
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
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/acs.jmedchem.8b00265
DB00747 12758 None 5 Human Binding pIC50 = 9.2 9.2 -12 9
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
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/acs.jmedchem.8b00265
1734 116 None 10 Human Binding pIC50 = 9.2 9.2 -1 12
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 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 None 10 Human Binding pIC50 = 9.2 9.2 -1 12
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 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 None 10 Human Binding pIC50 = 9.2 9.2 -1 12
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 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
49800047 14483 None 1 Human Binding pIC50 = 9.2 9.2 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14483 None 1 Human Binding pIC50 = 9.2 9.2 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14483 None 1 Human Binding pIC50 = 9.2 9.2 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
174174 523 None 49 Human Binding pIC50 = 9.1 9.1 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
174174.0 523 None 49 Human Binding pIC50 = 9.1 9.1 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
260 523 None 49 Human Binding pIC50 = 9.1 9.1 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
320 523 None 49 Human Binding pIC50 = 9.1 9.1 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 523 None 49 Human Binding pIC50 = 9.1 9.1 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 523 None 49 Human Binding pIC50 = 9.1 9.1 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 None 10 Human Binding pIC50 = 9.1 9.1 -1 12
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 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 None 10 Human Binding pIC50 = 9.1 9.1 -1 12
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 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 None 10 Human Binding pIC50 = 9.1 9.1 -1 12
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 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
1734 116 None 10 Human Binding pIC50 = 9.0 9.0 -1 12
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
307 116 None 10 Human Binding pIC50 = 9.0 9.0 -1 12
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
CHEMBL168067 116 None 10 Human Binding pIC50 = 9.0 9.0 -1 12
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
2200 3131 None 46 Human Binding pIC50 = 8.9 8.9 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
328 3131 None 46 Human Binding pIC50 = 8.9 8.9 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
4848 3131 None 46 Human Binding pIC50 = 8.9 8.9 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
4848.0 3131 None 46 Human Binding pIC50 = 8.9 8.9 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
CHEMBL9967 3131 None 46 Human Binding pIC50 = 8.9 8.9 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
DB00670 3131 None 46 Human Binding pIC50 = 8.9 8.9 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
11968014 12758 None 5 Human Binding pIC50 = 8.9 8.9 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
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/jm501173q
119680147.0 12758 None 5 Human Binding pIC50 = 8.9 8.9 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
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/jm501173q
CHEMBL1187846 12758 None 5 Human Binding pIC50 = 8.9 8.9 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
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/jm501173q
DB00747 12758 None 5 Human Binding pIC50 = 8.9 8.9 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
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/jm501173q
1734 116 None 10 Human Binding pIC50 = 8.7 8.7 -1 12
Percent inhibition against Muscarinic acetylcholine receptor M4 at 1 uMPercent inhibition against Muscarinic acetylcholine receptor M4 at 1 uM
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm058018d
307 116 None 10 Human Binding pIC50 = 8.7 8.7 -1 12
Percent inhibition against Muscarinic acetylcholine receptor M4 at 1 uMPercent inhibition against Muscarinic acetylcholine receptor M4 at 1 uM
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm058018d
CHEMBL168067 116 None 10 Human Binding pIC50 = 8.7 8.7 -1 12
Percent inhibition against Muscarinic acetylcholine receptor M4 at 1 uMPercent inhibition against Muscarinic acetylcholine receptor M4 at 1 uM
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm058018d
2028 2979 None 80 Human Binding pIC50 = 8.7 8.7 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 2979 None 80 Human Binding pIC50 = 8.7 8.7 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 2979 None 80 Human Binding pIC50 = 8.7 8.7 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634.0 2979 None 80 Human Binding pIC50 = 8.7 8.7 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 2979 None 80 Human Binding pIC50 = 8.7 8.7 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 2979 None 80 Human Binding pIC50 = 8.7 8.7 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
44575653 181644 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
ChEMBL 327 14 7 4 0.4 N=C(N)NCCCCCCCCC(=O)C(N)CCCNC(=N)N 10.1021/np50120a004
CHEMBL477542 181644 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
ChEMBL 327 14 7 4 0.4 N=C(N)NCCCCCCCCC(=O)C(N)CCCNC(=N)N 10.1021/np50120a004
49671356 157425 None 10 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at human muscarinic M4 receptorAntagonist activity at human muscarinic M4 receptor
ChEMBL 435 4 0 6 3.0 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4078704 157425 None 10 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at human muscarinic M4 receptorAntagonist activity at human muscarinic M4 receptor
ChEMBL 435 4 0 6 3.0 CC1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
2551 794 None 23 Human Binding pIC50 = 6 6.0 -21 11
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
2551.0 794 None 23 Human Binding pIC50 = 6 6.0 -21 11
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
298 794 None 23 Human Binding pIC50 = 6 6.0 -21 11
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
488 794 None 23 Human Binding pIC50 = 6 6.0 -21 11
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
CHEMBL965 794 None 23 Human Binding pIC50 = 6 6.0 -21 11
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
DB00411 794 None 23 Human Binding pIC50 = 6 6.0 -21 11
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
14660293 52653 None 3 Human Binding pIC50 = 4 4.0 - 0
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2 10.1021/jm9705216
CHEMBL15936 52653 None 3 Human Binding pIC50 = 4 4.0 - 0
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2 10.1021/jm9705216
11057 176149 None 23 Human Binding pIC50 = 6 6.0 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 176149 None 23 Human Binding pIC50 = 6 6.0 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 176149 None 23 Human Binding pIC50 = 6 6.0 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 176149 None 23 Human Binding pIC50 = 6 6.0 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
1530 2182 None 50 Human Binding pIC50 = 6 6.0 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2182 None 50 Human Binding pIC50 = 6 6.0 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827.0 2182 None 50 Human Binding pIC50 = 6 6.0 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2182 None 50 Human Binding pIC50 = 6 6.0 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2182 None 50 Human Binding pIC50 = 6 6.0 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2182 None 50 Human Binding pIC50 = 6 6.0 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
5282593 55258 None 26 Human Binding pIC50 = 7 7.0 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 55258 None 26 Human Binding pIC50 = 7 7.0 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 55258 None 26 Human Binding pIC50 = 7 7.0 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10777692 11427 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180296 11427 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL120539 11427 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
3013846 188239 None 2 Human Binding pIC50 = 6.0 6.0 -1 5
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 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 188239 None 2 Human Binding pIC50 = 6.0 6.0 -1 5
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 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
2200 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
328 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
4848 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
4848.0 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
CHEMBL9967 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
DB00670 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
2200 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
328 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
4848 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
4848.0 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
CHEMBL9967 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
DB00670 3131 None 46 Human Binding pIC50 = 6.0 6.0 -2 12
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm501173q
2683 102888 None 25 Human Binding pIC50 = 7.0 7.0 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102888 None 25 Human Binding pIC50 = 7.0 7.0 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102888 None 25 Human Binding pIC50 = 7.0 7.0 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
10567192 12096 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12096 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12096 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
10678449 22653 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 154 2 0 3 0.6 CO/N=C/[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL132698 22653 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 154 2 0 3 0.6 CO/N=C/[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
10593954 13076 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 13076 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 13076 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
324 1925 None 15 Human Binding pIC50 = 6.9 6.9 -1 9
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 1925 None 15 Human Binding pIC50 = 6.9 6.9 -1 9
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 1925 None 15 Human Binding pIC50 = 6.9 6.9 -1 9
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
10784004 13387 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1192621 13387 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL543890 13387 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
10522202 11434 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180312 11434 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL121385 11434 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
2812 4779 None 101 Human Binding pIC50 = 4.9 4.9 -19 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4779 None 101 Human Binding pIC50 = 4.9 4.9 -19 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
107782 14468 None 18 Human Binding pIC50 = 4.9 4.9 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14468 None 18 Human Binding pIC50 = 4.9 4.9 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14468 None 18 Human Binding pIC50 = 4.9 4.9 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10082470 52717 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
CHEMBL15944 52717 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
CHEMBL308608 52717 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
14925759 158038 None 6 Human Binding pIC50 = 4.9 4.9 -3235 13
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 158038 None 6 Human Binding pIC50 = 4.9 4.9 -3235 13
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
137640201 156961 None 2 Human Binding pIC50 = 5.9 5.9 -575 13
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156961 None 2 Human Binding pIC50 = 5.9 5.9 -575 13
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
118719926 115780 None 0 Human Binding pIC50 = 4.9 4.9 -102 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 115780 None 0 Human Binding pIC50 = 4.9 4.9 -102 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
4601 206747 None 35 Human Binding pIC50 = 6.9 6.9 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
4601.0 206747 None 35 Human Binding pIC50 = 6.9 6.9 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 206747 None 35 Human Binding pIC50 = 6.9 6.9 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 206747 None 35 Human Binding pIC50 = 6.9 6.9 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
DB01173 206747 None 35 Human Binding pIC50 = 6.9 6.9 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
10854879 11417 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180239 11417 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL118241 11417 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
153284501 176139 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Antagonist activity at human Gs/Gi/o-coupled CHRM4 expressed in CHOK1 cells assessed as inhibition in acetylcholine-induced beta-arrestin 2 recruitment incubated for 30 mins followed by acetylcholine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human Gs/Gi/o-coupled CHRM4 expressed in CHOK1 cells assessed as inhibition in acetylcholine-induced beta-arrestin 2 recruitment incubated for 30 mins followed by acetylcholine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay
ChEMBL 480 5 1 5 4.4 CC[C@@]12CCCN3CCc4c([nH]c5ccccc45)[C@]31N(Cc1cn(Cc3ccccc3)nn1)C(=O)C2 10.1021/acs.jmedchem.9b01924
CHEMBL4592258 176139 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Antagonist activity at human Gs/Gi/o-coupled CHRM4 expressed in CHOK1 cells assessed as inhibition in acetylcholine-induced beta-arrestin 2 recruitment incubated for 30 mins followed by acetylcholine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human Gs/Gi/o-coupled CHRM4 expressed in CHOK1 cells assessed as inhibition in acetylcholine-induced beta-arrestin 2 recruitment incubated for 30 mins followed by acetylcholine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay
ChEMBL 480 5 1 5 4.4 CC[C@@]12CCCN3CCc4c([nH]c5ccccc45)[C@]31N(Cc1cn(Cc3ccccc3)nn1)C(=O)C2 10.1021/acs.jmedchem.9b01924
10538337 12111 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12111 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12111 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1 10.1021/jm980067l
10641009 11426 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180292 11426 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL120472 11426 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
44190762 176880 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of radioligand from muscarinic M4 receptorDisplacement of radioligand from muscarinic M4 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 176880 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of radioligand from muscarinic M4 receptorDisplacement of radioligand from muscarinic M4 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
2230 465 None 60 Human Binding pIC50 = 4.9 4.9 -218 10
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
296 465 None 60 Human Binding pIC50 = 4.9 4.9 -218 10
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
CHEMBL7303 465 None 60 Human Binding pIC50 = 4.9 4.9 -218 10
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
DB04365 465 None 60 Human Binding pIC50 = 4.9 4.9 -218 10
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
2274 3173 None 58 Human Binding pIC50 = 5.9 5.9 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 None 58 Human Binding pIC50 = 5.9 5.9 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917.0 3173 None 58 Human Binding pIC50 = 5.9 5.9 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 None 58 Human Binding pIC50 = 5.9 5.9 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 None 58 Human Binding pIC50 = 5.9 5.9 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 None 58 Human Binding pIC50 = 5.9 5.9 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
10610375 11422 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL1180284 11422 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL120109 11422 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
10610375 11422 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 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 11422 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 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 11422 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 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
6075 150108 None 42 Human Binding pIC50 = 6.9 6.9 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150108 None 42 Human Binding pIC50 = 6.9 6.9 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
441383 20333 None 57 Human Binding pIC50 = 4.9 4.9 -5 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 20333 None 57 Human Binding pIC50 = 4.9 4.9 -5 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10760249 11423 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 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 11423 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 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 11423 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 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 11423 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11423 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11423 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
10636001 11425 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11425 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11425 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
9905467 11436 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180316 11436 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL121520 11436 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
118719922 115775 None 0 Human Binding pIC50 = 6.8 6.8 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 115775 None 0 Human Binding pIC50 = 6.8 6.8 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
164606754 184702 None 7 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4850236 184702 None 7 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873617 184702 None 7 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 5 4.1 Fc1cc(F)c(F)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
10759393 84385 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 84385 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 84385 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
10846833 49805 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 225 0 0 5 1.7 CN1CCC2=C(C1)c1nsnc1SC2 10.1021/jm9705216
CHEMBL15675 49805 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 225 0 0 5 1.7 CN1CCC2=C(C1)c1nsnc1SC2 10.1021/jm9705216
10663572 13159 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 13159 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 13159 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
44302833 102501 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 102501 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
118719927 115781 None 0 Human Binding pIC50 = 5.8 5.8 -3 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354074 115781 None 0 Human Binding pIC50 = 5.8 5.8 -3 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
2726 919 None 68 Human Binding pIC50 = 6.8 6.8 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
2726.0 919 None 68 Human Binding pIC50 = 6.8 6.8 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 None 68 Human Binding pIC50 = 6.8 6.8 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 None 68 Human Binding pIC50 = 6.8 6.8 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 None 68 Human Binding pIC50 = 6.8 6.8 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 None 68 Human Binding pIC50 = 6.8 6.8 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
44302755 202676 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 202676 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
9913341 82158 None 4 Human Binding pIC50 = 7.8 7.8 3 5
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determinedInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determined
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL216927 82158 None 4 Human Binding pIC50 = 7.8 7.8 3 5
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determinedInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determined
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL553058 82158 None 4 Human Binding pIC50 = 7.8 7.8 3 5
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determinedInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determined
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
135398745 2914 None 112 Human Binding pIC50 = 6.8 6.8 -32 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
135398745.0 2914 None 112 Human Binding pIC50 = 6.8 6.8 -32 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2914 None 112 Human Binding pIC50 = 6.8 6.8 -32 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2914 None 112 Human Binding pIC50 = 6.8 6.8 -32 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2914 None 112 Human Binding pIC50 = 6.8 6.8 -32 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
60838 183874 None 99 Human Binding pIC50 = 5.8 5.8 1 2
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
CHEMBL481 183874 None 99 Human Binding pIC50 = 5.8 5.8 1 2
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
10522336 15130 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.3 CCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL120972 15130 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.3 CCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
2337 3256 None 77 Human Binding pIC50 = 5.8 5.8 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3256 None 77 Human Binding pIC50 = 5.8 5.8 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3256 None 77 Human Binding pIC50 = 5.8 5.8 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002.0 3256 None 77 Human Binding pIC50 = 5.8 5.8 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3256 None 77 Human Binding pIC50 = 5.8 5.8 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3256 None 77 Human Binding pIC50 = 5.8 5.8 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
46871844 6812 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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 6812 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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
4735 195115 None 96 Human Binding pIC50 = 5.8 5.8 -6 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL361506 195115 None 96 Human Binding pIC50 = 5.8 5.8 -6 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL55 195115 None 96 Human Binding pIC50 = 5.8 5.8 -6 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
46871665 6595 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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 6595 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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
277 1301 None 62 Human Binding pIC50 = 7.8 7.8 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1301 None 62 Human Binding pIC50 = 7.8 7.8 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913.0 1301 None 62 Human Binding pIC50 = 7.8 7.8 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1301 None 62 Human Binding pIC50 = 7.8 7.8 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1301 None 62 Human Binding pIC50 = 7.8 7.8 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1301 None 62 Human Binding pIC50 = 7.8 7.8 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
118719926 115780 None 0 Human Binding pIC50 = 5.8 5.8 -102 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 115780 None 0 Human Binding pIC50 = 5.8 5.8 -102 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
2750 204061 None 76 Human Binding pIC50 = 4.8 4.8 -1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 204061 None 76 Human Binding pIC50 = 4.8 4.8 -1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
44302775 202796 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 202796 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
1548953 207679 None 27 Human Binding pIC50 = 5.8 5.8 -1 17
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 207679 None 27 Human Binding pIC50 = 5.8 5.8 -1 17
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
10782462 12114 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12114 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12114 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL5287400 194383 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Positive allosteric modulator activity at human M4 receptorPositive allosteric modulator activity at human M4 receptor
ChEMBL 417 5 0 6 5.2 COc1cc2ccc(-c3nc(C)ccc3-c3cnn(CC4(F)CCCC4)c3)cc2nn1 10.1039/D1MD00096A
191 403 None 98 Human Binding pIC50 = 5.8 5.8 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 403 None 98 Human Binding pIC50 = 5.8 5.8 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 403 None 98 Human Binding pIC50 = 5.8 5.8 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170.0 403 None 98 Human Binding pIC50 = 5.8 5.8 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 403 None 98 Human Binding pIC50 = 5.8 5.8 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 403 None 98 Human Binding pIC50 = 5.8 5.8 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
10664532 12112 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12112 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12112 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
10569816 11459 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11459 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11459 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
10236758 115772 None 5 Human Binding pIC50 = 6.8 6.8 -213 13
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 115772 None 5 Human Binding pIC50 = 6.8 6.8 -213 13
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
2247 505 None 81 Human Binding pIC50 = 5.7 5.7 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 None 81 Human Binding pIC50 = 5.7 5.7 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 None 81 Human Binding pIC50 = 5.7 5.7 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 None 81 Human Binding pIC50 = 5.7 5.7 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 None 81 Human Binding pIC50 = 5.7 5.7 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
118719922 115775 None 0 Human Binding pIC50 = 5.7 5.7 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 115775 None 0 Human Binding pIC50 = 5.7 5.7 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
10594386 11418 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11418 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11418 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
1210 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
1213 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2725 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036.0 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
4411 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
616 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
6976 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
716121 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 918 None 51 Human Binding pIC50 = 5.7 5.7 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
237 204865 None 48 Human Binding pIC50 = 5.7 5.7 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 204865 None 48 Human Binding pIC50 = 5.7 5.7 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 204865 None 48 Human Binding pIC50 = 5.7 5.7 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 204865 None 48 Human Binding pIC50 = 5.7 5.7 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
23724781.0 2835 None 19 Human Binding pIC50 = 8.6 8.6 -9 9
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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
316 2835 None 19 Human Binding pIC50 = 8.6 8.6 -9 9
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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 2835 None 19 Human Binding pIC50 = 8.6 8.6 -9 9
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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 2835 None 19 Human Binding pIC50 = 8.6 8.6 -9 9
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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
CHEMBL1354199 2835 None 19 Human Binding pIC50 = 8.6 8.6 -9 9
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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 2835 None 19 Human Binding pIC50 = 8.6 8.6 -9 9
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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 2835 None 19 Human Binding pIC50 = 8.6 8.6 -9 9
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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 2835 None 19 Human Binding pIC50 = 8.6 8.6 -9 9
Compound was evaluated for its binding affinity at human muscarinic receptor m4 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 m4 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
1201549 597 None 24 Human Binding pIC50 = 8.6 8.6 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
1201549.0 597 None 24 Human Binding pIC50 = 8.6 8.6 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
333 597 None 24 Human Binding pIC50 = 8.6 8.6 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 597 None 24 Human Binding pIC50 = 8.6 8.6 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 597 None 24 Human Binding pIC50 = 8.6 8.6 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 597 None 24 Human Binding pIC50 = 8.6 8.6 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 597 None 24 Human Binding pIC50 = 8.6 8.6 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
3042 1414 None 35 Human Binding pIC50 = 8.5 8.5 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
3042.0 1414 None 35 Human Binding pIC50 = 8.5 8.5 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1414 None 35 Human Binding pIC50 = 8.5 8.5 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1414 None 35 Human Binding pIC50 = 8.5 8.5 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1414 None 35 Human Binding pIC50 = 8.5 8.5 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1414 None 35 Human Binding pIC50 = 8.5 8.5 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
26987 949 None 33 Human Binding pIC50 = 7.7 7.7 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
26987.0 949 None 33 Human Binding pIC50 = 7.7 7.7 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 949 None 33 Human Binding pIC50 = 7.7 7.7 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 949 None 33 Human Binding pIC50 = 7.7 7.7 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 949 None 33 Human Binding pIC50 = 7.7 7.7 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 949 None 33 Human Binding pIC50 = 7.7 7.7 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
10567372 12131 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12131 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12131 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12131 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
44302900 202798 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 202798 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
135 2532 None 43 Human Binding pIC50 = 5.7 5.7 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2532 None 43 Human Binding pIC50 = 5.7 5.7 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2532 None 43 Human Binding pIC50 = 5.7 5.7 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184.0 2532 None 43 Human Binding pIC50 = 5.7 5.7 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2532 None 43 Human Binding pIC50 = 5.7 5.7 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2532 None 43 Human Binding pIC50 = 5.7 5.7 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
3198 205513 None 76 Human Binding pIC50 = 5.7 5.7 -8 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205513 None 76 Human Binding pIC50 = 5.7 5.7 -8 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205513 None 76 Human Binding pIC50 = 5.7 5.7 -8 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
10547222 114786 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333940 114786 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10592484 11435 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180314 11435 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL121476 11435 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10666533 11432 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11432 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11432 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
10236758 115772 None 5 Human Binding pIC50 = 5.7 5.7 -213 13
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 115772 None 5 Human Binding pIC50 = 5.7 5.7 -213 13
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
10499832 12135 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12135 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12135 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
43815 186920 None 64 Human Binding pIC50 = 6.6 6.6 -8 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 186920 None 64 Human Binding pIC50 = 6.6 6.6 -8 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 186920 None 64 Human Binding pIC50 = 6.6 6.6 -8 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
101882890 115776 None 0 Human Binding pIC50 = 5.6 5.6 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354069 115776 None 0 Human Binding pIC50 = 5.6 5.6 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
2200 3131 None 46 Human Binding pIC50 = 6.6 6.6 -2 12
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 3131 None 46 Human Binding pIC50 = 6.6 6.6 -2 12
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 3131 None 46 Human Binding pIC50 = 6.6 6.6 -2 12
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
4848.0 3131 None 46 Human Binding pIC50 = 6.6 6.6 -2 12
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 3131 None 46 Human Binding pIC50 = 6.6 6.6 -2 12
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 3131 None 46 Human Binding pIC50 = 6.6 6.6 -2 12
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
2774 3868 None 95 Human Binding pIC50 = 7.6 7.6 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
5593 3868 None 95 Human Binding pIC50 = 7.6 7.6 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
5593.0 3868 None 95 Human Binding pIC50 = 7.6 7.6 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
7319 3868 None 95 Human Binding pIC50 = 7.6 7.6 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
CHEMBL1200604 3868 None 95 Human Binding pIC50 = 7.6 7.6 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB00809 3868 None 95 Human Binding pIC50 = 7.6 7.6 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB01199 3868 None 95 Human Binding pIC50 = 7.6 7.6 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
3652 4097 None 79 Human Binding pIC50 = 7.6 7.6 -3 18
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
57 4097 None 79 Human Binding pIC50 = 7.6 7.6 -3 18
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
60809 4097 None 79 Human Binding pIC50 = 7.6 7.6 -3 18
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
60809.0 4097 None 79 Human Binding pIC50 = 7.6 7.6 -3 18
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
CHEMBL21536 4097 None 79 Human Binding pIC50 = 7.6 7.6 -3 18
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
DB15357 4097 None 79 Human Binding pIC50 = 7.6 7.6 -3 18
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsInhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
2335 11848 None 22 Human Binding pIC50 = 6.6 6.6 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 11848 None 22 Human Binding pIC50 = 6.6 6.6 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 11848 None 22 Human Binding pIC50 = 6.6 6.6 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 11848 None 22 Human Binding pIC50 = 6.6 6.6 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10854880 11421 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11421 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11421 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
5648 78411 None 9 Human Binding pIC50 = 7.6 7.6 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 78411 None 9 Human Binding pIC50 = 7.6 7.6 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 78411 None 9 Human Binding pIC50 = 7.6 7.6 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
68617 205527 None 62 Human Binding pIC50 = 5.6 5.6 -20 26
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 205527 None 62 Human Binding pIC50 = 5.6 5.6 -20 26
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 205527 None 62 Human Binding pIC50 = 5.6 5.6 -20 26
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
44302834 202710 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 202710 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
3055 1433 None 44 Human Binding pIC50 = 6.6 6.6 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
313 1433 None 44 Human Binding pIC50 = 6.6 6.6 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
7163 1433 None 44 Human Binding pIC50 = 6.6 6.6 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
CHEMBL936 1433 None 44 Human Binding pIC50 = 6.6 6.6 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
DB01231 1433 None 44 Human Binding pIC50 = 6.6 6.6 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
10808719 12132 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184120 12132 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL333125 12132 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
10546275 15202 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 15202 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.5 CCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL5287400 194383 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Positive allosteric modulator activity at rat M4 receptor by FLIPR assayPositive allosteric modulator activity at rat M4 receptor by FLIPR assay
ChEMBL 417 5 0 6 5.2 COc1cc2ccc(-c3nc(C)ccc3-c3cnn(CC4(F)CCCC4)c3)cc2nn1 10.1039/D1MD00096A
2284 3182 None 33 Human Binding pIC50 = 6.5 6.5 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3182 None 33 Human Binding pIC50 = 6.5 6.5 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3182 None 33 Human Binding pIC50 = 6.5 6.5 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3182 None 33 Human Binding pIC50 = 6.5 6.5 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3182 None 33 Human Binding pIC50 = 6.5 6.5 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
11968014 12758 None 5 Human Binding pIC50 = 8.4 8.4 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
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/jm501173q
119680147.0 12758 None 5 Human Binding pIC50 = 8.4 8.4 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
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/jm501173q
CHEMBL1187846 12758 None 5 Human Binding pIC50 = 8.4 8.4 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
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/jm501173q
DB00747 12758 None 5 Human Binding pIC50 = 8.4 8.4 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
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/jm501173q
11968014 12758 None 5 Human Binding pIC50 = 8.4 8.4 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
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/jm501173q
119680147.0 12758 None 5 Human Binding pIC50 = 8.4 8.4 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
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/jm501173q
CHEMBL1187846 12758 None 5 Human Binding pIC50 = 8.4 8.4 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
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/jm501173q
DB00747 12758 None 5 Human Binding pIC50 = 8.4 8.4 -12 9
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
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/jm501173q
25070582 61454 None 28 Human Binding pIC50 = 6.5 6.5 - 1
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61454 None 28 Human Binding pIC50 = 6.5 6.5 - 1
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
44302728 198713 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 198713 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
10518821 12127 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12127 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12127 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
46891179 6417 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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 6417 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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
46871666 7069 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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 7069 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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
4189 206922 None 96 Human Binding pIC50 = 5.5 5.5 -10 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206922 None 96 Human Binding pIC50 = 5.5 5.5 -10 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206922 None 96 Human Binding pIC50 = 5.5 5.5 -10 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
10611310 12123 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12123 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12123 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
124 2981 None 47 Human Binding pIC50 = 5.5 5.5 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2981 None 47 Human Binding pIC50 = 5.5 5.5 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2981 None 47 Human Binding pIC50 = 5.5 5.5 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636.0 2981 None 47 Human Binding pIC50 = 5.5 5.5 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2981 None 47 Human Binding pIC50 = 5.5 5.5 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2981 None 47 Human Binding pIC50 = 5.5 5.5 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
9882189 167434 None 33 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to muscarinic 4 receptor (unknown origin)Binding affinity to muscarinic 4 receptor (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1016/j.bmc.2022.117032
CHEMBL4297224 167434 None 33 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to muscarinic 4 receptor (unknown origin)Binding affinity to muscarinic 4 receptor (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1016/j.bmc.2022.117032
9882189 167434 None 33 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01192
CHEMBL4297224 167434 None 33 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01192
118719926 115780 None 0 Human Binding pIC50 = 5.5 5.5 -102 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 115780 None 0 Human Binding pIC50 = 5.5 5.5 -102 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
5310989 200877 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 200877 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
124087 1389 None 114 Human Binding pIC50 = 6.5 6.5 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
124087.0 1389 None 114 Human Binding pIC50 = 6.5 6.5 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1389 None 114 Human Binding pIC50 = 6.5 6.5 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1389 None 114 Human Binding pIC50 = 6.5 6.5 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1389 None 114 Human Binding pIC50 = 6.5 6.5 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1389 None 114 Human Binding pIC50 = 6.5 6.5 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
1212 1662 None 50 Human Binding pIC50 = 5.5 5.5 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1662 None 50 Human Binding pIC50 = 5.5 5.5 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1662 None 50 Human Binding pIC50 = 5.5 5.5 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372.0 1662 None 50 Human Binding pIC50 = 5.5 5.5 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1662 None 50 Human Binding pIC50 = 5.5 5.5 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1662 None 50 Human Binding pIC50 = 5.5 5.5 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
118719921 115774 None 0 Human Binding pIC50 = 6.5 6.5 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 115774 None 0 Human Binding pIC50 = 6.5 6.5 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
44302741 202655 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 202655 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
4746 204891 None 31 Human Binding pIC50 = 5.5 5.5 1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL1334033 204891 None 31 Human Binding pIC50 = 5.5 5.5 1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL75880 204891 None 31 Human Binding pIC50 = 5.5 5.5 1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
176 398 None 66 Human Binding pIC50 = 5.4 5.4 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pIC50 = 5.4 5.4 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
2157.0 398 None 66 Human Binding pIC50 = 5.4 5.4 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pIC50 = 5.4 5.4 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pIC50 = 5.4 5.4 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pIC50 = 5.4 5.4 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
118719928 115782 None 0 Human Binding pIC50 = 5.4 5.4 1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354075 115782 None 0 Human Binding pIC50 = 5.4 5.4 1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
1547484 940 None 74 Human Binding pIC50 = 5.4 5.4 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
1547484.0 940 None 74 Human Binding pIC50 = 5.4 5.4 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 940 None 74 Human Binding pIC50 = 5.4 5.4 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 940 None 74 Human Binding pIC50 = 5.4 5.4 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 940 None 74 Human Binding pIC50 = 5.4 5.4 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 940 None 74 Human Binding pIC50 = 5.4 5.4 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
10358345 11442 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11442 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11442 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
44302813 101930 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 101930 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
1224 1432 None 83 Human Binding pIC50 = 6.4 6.4 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1432 None 83 Human Binding pIC50 = 6.4 6.4 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100.0 1432 None 83 Human Binding pIC50 = 6.4 6.4 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1432 None 83 Human Binding pIC50 = 6.4 6.4 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1432 None 83 Human Binding pIC50 = 6.4 6.4 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1432 None 83 Human Binding pIC50 = 6.4 6.4 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1432 None 83 Human Binding pIC50 = 6.4 6.4 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
10516408 11441 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180330 11441 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL122353 11441 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
3168 9262 None 92 Human Binding pIC50 = 5.4 5.4 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
3168.0 9262 None 92 Human Binding pIC50 = 5.4 5.4 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9262 None 92 Human Binding pIC50 = 5.4 5.4 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
DB00450 9262 None 92 Human Binding pIC50 = 5.4 5.4 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
5318 15576 None 49 Human Binding pIC50 = 5.4 5.4 1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15576 None 49 Human Binding pIC50 = 5.4 5.4 1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15576 None 49 Human Binding pIC50 = 5.4 5.4 1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
46890977 6732 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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 6732 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
118719922 115775 None 0 Human Binding pIC50 = 6.4 6.4 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 115775 None 0 Human Binding pIC50 = 6.4 6.4 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
4011 82408 None 49 Human Binding pIC50 = 6.4 6.4 -11 24
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82408 None 49 Human Binding pIC50 = 6.4 6.4 -11 24
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
10549581 11449 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11449 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11449 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
3158 56267 None 27 Human Binding pIC50 = 7.4 7.4 -40 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
3158.0 56267 None 27 Human Binding pIC50 = 7.4 7.4 -40 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56267 None 27 Human Binding pIC50 = 7.4 7.4 -40 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
DB01142 56267 None 27 Human Binding pIC50 = 7.4 7.4 -40 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
10595006 11445 None 0 Human Binding pIC50 = 4.4 4.4 -10 5
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11445 None 0 Human Binding pIC50 = 4.4 4.4 -10 5
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11445 None 0 Human Binding pIC50 = 4.4 4.4 -10 5
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11445 None 0 Human Binding pIC50 = 4.4 4.4 -10 5
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 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 11445 None 0 Human Binding pIC50 = 4.4 4.4 -10 5
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 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 11445 None 0 Human Binding pIC50 = 4.4 4.4 -10 5
Binding affinity to human M4 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M4 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
10757736 14504 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 14504 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
10851853 12188 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12188 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12188 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
118719921 115774 None 0 Human Binding pIC50 = 6.4 6.4 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 115774 None 0 Human Binding pIC50 = 6.4 6.4 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
135398737 958 None 93 Human Binding pIC50 = 7.4 7.4 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
135398737.0 958 None 93 Human Binding pIC50 = 7.4 7.4 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 None 93 Human Binding pIC50 = 7.4 7.4 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 None 93 Human Binding pIC50 = 7.4 7.4 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 None 93 Human Binding pIC50 = 7.4 7.4 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 None 93 Human Binding pIC50 = 7.4 7.4 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
657255 199084 None 34 Human Binding pIC50 = 5.3 5.3 -9 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 199084 None 34 Human Binding pIC50 = 5.3 5.3 -9 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
44302776 102350 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 102350 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
10591874 13316 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1192001 13316 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL543177 13316 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
44302793 199729 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 199729 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
2230 465 None 60 Human Binding pIC50 = 4.3 4.3 -218 10
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
296 465 None 60 Human Binding pIC50 = 4.3 4.3 -218 10
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
CHEMBL7303 465 None 60 Human Binding pIC50 = 4.3 4.3 -218 10
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
DB04365 465 None 60 Human Binding pIC50 = 4.3 4.3 -218 10
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
10236758 115772 None 5 Human Binding pIC50 = 4.3 4.3 -213 13
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 115772 None 5 Human Binding pIC50 = 4.3 4.3 -213 13
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
57396813 71545 None 0 Human Binding pIC50 = 5.3 5.3 - 5
Inhibition of M4 receptorInhibition of M4 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71545 None 0 Human Binding pIC50 = 5.3 5.3 - 5
Inhibition of M4 receptorInhibition of M4 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71545 None 0 Human Binding pIC50 = 5.3 5.3 - 5
Inhibition of M4 receptorInhibition of M4 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
1016 3747 None 78 Human Binding pIC50 = 5.3 5.3 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pIC50 = 5.3 5.3 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pIC50 = 5.3 5.3 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pIC50 = 5.3 5.3 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pIC50 = 5.3 5.3 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pIC50 = 5.3 5.3 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
10797864 26145 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 1.0 CO/N=C(\C#N)C12CCCN(CC1)C2 10.1021/jm9702903
CHEMBL135645 26145 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 1.0 CO/N=C(\C#N)C12CCCN(CC1)C2 10.1021/jm9702903
10726038 119432 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.6 CO/N=C(\C#N)C12CCN(CC1)C2 10.1021/jm9702903
CHEMBL344892 119432 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.6 CO/N=C(\C#N)C12CCN(CC1)C2 10.1021/jm9702903
656392 183800 None 3 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 183800 None 3 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
180 401 None 56 Human Binding pIC50 = 8.3 8.3 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 None 56 Human Binding pIC50 = 8.3 8.3 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 None 56 Human Binding pIC50 = 8.3 8.3 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160.0 401 None 56 Human Binding pIC50 = 8.3 8.3 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 None 56 Human Binding pIC50 = 8.3 8.3 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 None 56 Human Binding pIC50 = 8.3 8.3 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
11968014 12758 None 5 Human Binding pIC50 = 8.3 8.3 -12 9
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
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/acs.jmedchem.8b00265
119680147.0 12758 None 5 Human Binding pIC50 = 8.3 8.3 -12 9
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
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/acs.jmedchem.8b00265
CHEMBL1187846 12758 None 5 Human Binding pIC50 = 8.3 8.3 -12 9
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
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/acs.jmedchem.8b00265
DB00747 12758 None 5 Human Binding pIC50 = 8.3 8.3 -12 9
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
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/acs.jmedchem.8b00265
2745 3861 None 42 Human Binding pIC50 = 8.3 8.3 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572 3861 None 42 Human Binding pIC50 = 8.3 8.3 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572.0 3861 None 42 Human Binding pIC50 = 8.3 8.3 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
66007 3861 None 42 Human Binding pIC50 = 8.3 8.3 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
7315 3861 None 42 Human Binding pIC50 = 8.3 8.3 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
CHEMBL1490 3861 None 42 Human Binding pIC50 = 8.3 8.3 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
DB00376 3861 None 42 Human Binding pIC50 = 8.3 8.3 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
302 2977 None 25 Human Binding pIC50 = 5.3 5.3 -7 8
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
4630 2977 None 25 Human Binding pIC50 = 5.3 5.3 -7 8
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
CHEMBL7634 2977 None 25 Human Binding pIC50 = 5.3 5.3 -7 8
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
44302788 200622 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 200622 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
46891488 7173 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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 7173 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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
10567372 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10684720 12094 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12094 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12094 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
10567372 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10567372 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12131 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
12488 1657 None 56 Human Binding pIC50 = 5.3 5.3 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 1657 None 56 Human Binding pIC50 = 5.3 5.3 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 1657 None 56 Human Binding pIC50 = 5.3 5.3 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 1657 None 56 Human Binding pIC50 = 5.3 5.3 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10785471 113716 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 113716 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.9 CCCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
156493833 184907 None 2 Rat Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 7 3.6 Cn1cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2n1 10.1021/acsmedchemlett.1c00363
CHEMBL4853244 184907 None 2 Rat Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 432 5 1 7 3.6 Cn1cc2cc(-c3ccc(N[C@H]4C[C@@H]5CN(CC6CCOCC6)C[C@@H]5C4)nn3)ccc2n1 10.1021/acsmedchemlett.1c00363
10660 14416 None 58 Human Binding pIC50 = 6.2 6.2 -2 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10660.0 14416 None 58 Human Binding pIC50 = 6.2 6.2 -2 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
441281.0 14416 None 58 Human Binding pIC50 = 6.2 6.2 -2 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14416 None 58 Human Binding pIC50 = 6.2 6.2 -2 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
DB00985 14416 None 58 Human Binding pIC50 = 6.2 6.2 -2 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10686988 12189 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12189 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12189 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
118719927 115781 None 0 Human Binding pIC50 = 6.2 6.2 -3 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354074 115781 None 0 Human Binding pIC50 = 6.2 6.2 -3 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
118719928 115782 None 0 Human Binding pIC50 = 6.2 6.2 1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354075 115782 None 0 Human Binding pIC50 = 6.2 6.2 1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
164612139 184675 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 426 6 1 4 5.7 c1ccc(CN2CCC(CCNc3cc4c(nn3)-c3ccccc3CCCC4)CC2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4849905 184675 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from rat muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 426 6 1 4 5.7 c1ccc(CN2CCC(CCNc3cc4c(nn3)-c3ccccc3CCCC4)CC2)cc1 10.1021/acsmedchemlett.1c00363
2745 3861 None 42 Human Binding pIC50 = 8.2 8.2 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3861 None 42 Human Binding pIC50 = 8.2 8.2 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
5572.0 3861 None 42 Human Binding pIC50 = 8.2 8.2 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3861 None 42 Human Binding pIC50 = 8.2 8.2 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3861 None 42 Human Binding pIC50 = 8.2 8.2 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3861 None 42 Human Binding pIC50 = 8.2 8.2 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3861 None 42 Human Binding pIC50 = 8.2 8.2 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
44302727 101918 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 101918 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
10806268 12137 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12137 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12137 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
4841 67427 None 5 Human Binding pIC50 = 7.2 7.2 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 67427 None 5 Human Binding pIC50 = 7.2 7.2 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 67427 None 5 Human Binding pIC50 = 7.2 7.2 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
10267601 12129 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1184116 12129 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL332980 12129 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
118719921 115774 None 0 Human Binding pIC50 = 6.2 6.2 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 115774 None 0 Human Binding pIC50 = 6.2 6.2 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
10782321 12124 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
CHEMBL1184098 12124 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
CHEMBL332405 12124 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
4212 198679 None 82 Human Binding pIC50 = 6.2 6.2 -1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
CHEMBL1417019 198679 None 82 Human Binding pIC50 = 6.2 6.2 -1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
CHEMBL58 198679 None 82 Human Binding pIC50 = 6.2 6.2 -1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
10755732 12121 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184092 12121 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL332181 12121 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
9974222 11921 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1182709 11921 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL262198 11921 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
2286 3183 None 51 Human Binding pIC50 = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3183 None 51 Human Binding pIC50 = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927.0 3183 None 51 Human Binding pIC50 = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3183 None 51 Human Binding pIC50 = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3183 None 51 Human Binding pIC50 = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3183 None 51 Human Binding pIC50 = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
10638050 11415 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL116601 11415 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180202 11415 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
2551 794 None 23 Human Binding pIC50 = 5.1 5.1 -21 11
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
2551.0 794 None 23 Human Binding pIC50 = 5.1 5.1 -21 11
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
298 794 None 23 Human Binding pIC50 = 5.1 5.1 -21 11
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
488 794 None 23 Human Binding pIC50 = 5.1 5.1 -21 11
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
CHEMBL965 794 None 23 Human Binding pIC50 = 5.1 5.1 -21 11
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
DB00411 794 None 23 Human Binding pIC50 = 5.1 5.1 -21 11
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
49853884 90683 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity to M4 receptor (unknown origin) by radioligand displacement assayBinding affinity to M4 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 90683 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity to M4 receptor (unknown origin) by radioligand displacement assayBinding affinity to M4 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
10755733 11428 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11428 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11428 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
10761219 11431 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11431 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11431 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
10236758 115772 None 5 Human Binding pIC50 = 5.1 5.1 -213 13
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by beta-arrestin engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 115772 None 5 Human Binding pIC50 = 5.1 5.1 -213 13
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by beta-arrestin engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
10573693 11430 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11430 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11430 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
10852843 11924 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11924 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11924 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
118719927 115781 None 0 Human Binding pIC50 = 6.1 6.1 -3 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354074 115781 None 0 Human Binding pIC50 = 6.1 6.1 -3 8
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
46891076 6708 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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 6708 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 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
100 3805 None 58 Human Binding pIC50 = 7.1 7.1 -14 55
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3805 None 58 Human Binding pIC50 = 7.1 7.1 -14 55
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3805 None 58 Human Binding pIC50 = 7.1 7.1 -14 55
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3805 None 58 Human Binding pIC50 = 7.1 7.1 -14 55
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3805 None 58 Human Binding pIC50 = 7.1 7.1 -14 55
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
10487582 28229 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL137384 28229 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
44356367 118492 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 266 3 0 2 2.2 C[N+](C)(C)CC#CCOC(=O)c1cccc(Cl)c1 10.1021/jm9702903
CHEMBL341447 118492 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 266 3 0 2 2.2 C[N+](C)(C)CC#CCOC(=O)c1cccc(Cl)c1 10.1021/jm9702903
118719928 115782 None 0 Human Binding pIC50 = 6.1 6.1 1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354075 115782 None 0 Human Binding pIC50 = 6.1 6.1 1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
10688349 12136 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12136 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12136 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
3191 102858 None 97 Human Binding pIC50 = 6.1 6.1 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
3191.0 102858 None 97 Human Binding pIC50 = 6.1 6.1 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 102858 None 97 Human Binding pIC50 = 6.1 6.1 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
DB11742 102858 None 97 Human Binding pIC50 = 6.1 6.1 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10521205 11429 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11429 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11429 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
10829928 12402 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12402 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 12402 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1 10.1021/jm980067l
10614695 12157 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184188 12157 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL338280 12157 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
137640201 156961 None 2 Human Binding pIC50 = 5.1 5.1 -575 13
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156961 None 2 Human Binding pIC50 = 5.1 5.1 -575 13
Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
6726 1280 None 51 Human Binding pIC50 = 6.1 6.1 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
6726.0 1280 None 51 Human Binding pIC50 = 6.1 6.1 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1280 None 51 Human Binding pIC50 = 6.1 6.1 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1280 None 51 Human Binding pIC50 = 6.1 6.1 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1280 None 51 Human Binding pIC50 = 6.1 6.1 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1280 None 51 Human Binding pIC50 = 6.1 6.1 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
10827157 11437 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11437 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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 11437 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 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
306 3456 None 21 Human Binding pIC50 = 7.1 7.1 -2 5
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
3536 3456 None 21 Human Binding pIC50 = 7.1 7.1 -2 5
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
53930639 3456 None 21 Human Binding pIC50 = 7.1 7.1 -2 5
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
9577995 3456 None 21 Human Binding pIC50 = 7.1 7.1 -2 5
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
CHEMBL134641 3456 None 21 Human Binding pIC50 = 7.1 7.1 -2 5
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
11498 3019 None 41 Human Binding pIC50 = 7.0 7.0 38 6
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3019 None 41 Human Binding pIC50 = 7.0 7.0 38 6
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3019 None 41 Human Binding pIC50 = 7.0 7.0 38 6
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
2398 954 None 62 Human Binding pIC50 = 7.0 7.0 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 954 None 62 Human Binding pIC50 = 7.0 7.0 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801.0 954 None 62 Human Binding pIC50 = 7.0 7.0 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 954 None 62 Human Binding pIC50 = 7.0 7.0 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 954 None 62 Human Binding pIC50 = 7.0 7.0 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 954 None 62 Human Binding pIC50 = 7.0 7.0 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
10248541 182899 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
ChEMBL 369 15 7 4 0.5 CC(=O)NC(CCCNC(=N)N)C(=O)CCCCCCCCNC(=N)N 10.1021/np50120a004
CHEMBL479224 182899 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
ChEMBL 369 15 7 4 0.5 CC(=O)NC(CCCNC(=N)N)C(=O)CCCCCCCCNC(=N)N 10.1021/np50120a004
1971 2866 None 38 Human Binding pIC50 = 7.0 7.0 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2866 None 38 Human Binding pIC50 = 7.0 7.0 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2866 None 38 Human Binding pIC50 = 7.0 7.0 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543.0 2866 None 38 Human Binding pIC50 = 7.0 7.0 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2866 None 38 Human Binding pIC50 = 7.0 7.0 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2866 None 38 Human Binding pIC50 = 7.0 7.0 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
11793999 12115 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184074 12115 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL331516 12115 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
101882890 115776 None 0 Human Binding pIC50 = 4.0 4.0 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354069 115776 None 0 Human Binding pIC50 = 4.0 4.0 -1 5
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assayAntagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
164612139 184675 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 426 6 1 4 5.7 c1ccc(CN2CCC(CCNc3cc4c(nn3)-c3ccccc3CCCC4)CC2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4849905 184675 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysisDisplacement of [3H]NMS from human muscarinic receptor M4 expressed in CHO cell membranes incubated for 3 hrs by radiometric scintillation counting analysis
ChEMBL 426 6 1 4 5.7 c1ccc(CN2CCC(CCNc3cc4c(nn3)-c3ccccc3CCCC4)CC2)cc1 10.1021/acsmedchemlett.1c00363
44302901 101056 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 101056 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
10511551 25831 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL135328 25831 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@@H]1CN2CC[C@H]1C2 10.1021/jm9702903
44302879 202718 None 0 Human Binding pIC50 = 5 5.0 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 202718 None 0 Human Binding pIC50 = 5 5.0 - 0
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
164612037 185377 None 0 Human Binding pKd = 10.3 10.3 1 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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 185377 None 0 Human Binding pKd = 10.3 10.3 1 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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 192968 None 0 Human Binding pKd = 10.3 10.3 -3 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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 192968 None 0 Human Binding pKd = 10.3 10.3 -3 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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 192968 None 0 Human Binding pKd = 10.3 10.3 -3 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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 193019 None 0 Human Binding pKd = 10.3 10.3 1 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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 193019 None 0 Human Binding pKd = 10.3 10.3 1 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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 193019 None 0 Human Binding pKd = 10.3 10.3 1 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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 193031 None 0 Human Binding pKd = 10.3 10.3 1 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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 193031 None 0 Human Binding pKd = 10.3 10.3 1 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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 193031 None 0 Human Binding pKd = 10.3 10.3 1 20
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M4 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
10365181 18557 None 0 Rat Binding pKd = 9.5 9.5 1 3
In vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissueIn vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissue
ChEMBL 427 5 1 4 2.9 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(C/C=C/I)c1ccccc1 10.1021/jm00020a004
CHEMBL127587 18557 None 0 Rat Binding pKd = 9.5 9.5 1 3
In vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissueIn vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissue
ChEMBL 427 5 1 4 2.9 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(C/C=C/I)c1ccccc1 10.1021/jm00020a004
137630050 161040 None 0 Human Binding pKd = 9.2 9.2 -1 5
Binding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 hrs by liquid scintillation counting assayBinding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 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 161040 None 0 Human Binding pKd = 9.2 9.2 -1 5
Binding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 hrs by liquid scintillation counting assayBinding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 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 161040 None 0 Human Binding pKd = 9.2 9.2 -1 5
Binding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 hrs by liquid scintillation counting assayBinding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 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 161040 None 0 Human Binding pKd = 9.2 9.2 -1 5
Binding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 hrs by liquid scintillation counting assayBinding affinity to human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 2 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
10365181 18557 None 0 Rat Binding pKd = 8.6 8.6 1 3
In vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissueIn vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissue
ChEMBL 427 5 1 4 2.9 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(C/C=C/I)c1ccccc1 10.1021/jm00020a004
CHEMBL127587 18557 None 0 Rat Binding pKd = 8.6 8.6 1 3
In vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissueIn vitro binding affinity towards Muscarinic acetylcholine receptor M4 using [3H]QNB as radioligand from rat heart tissue
ChEMBL 427 5 1 4 2.9 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(C/C=C/I)c1ccccc1 10.1021/jm00020a004
156015807 178299 None 0 Human Binding pKd = 8.0 8.0 -3 5
Binding affinity to human muscarinic M4 receptor expressed in CHO-K9 cells incubated in dark at 22 degree C for 2 hrs by FACSCalibur flow cytometric saturation binding studyBinding affinity to human muscarinic M4 receptor expressed in CHO-K9 cells incubated in dark at 22 degree C for 2 hrs by FACSCalibur flow cytometric saturation binding study
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 178299 None 0 Human Binding pKd = 8.0 8.0 -3 5
Binding affinity to human muscarinic M4 receptor expressed in CHO-K9 cells incubated in dark at 22 degree C for 2 hrs by FACSCalibur flow cytometric saturation binding studyBinding affinity to human muscarinic M4 receptor expressed in CHO-K9 cells incubated in dark at 22 degree C for 2 hrs by FACSCalibur flow cytometric saturation binding study
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 178299 None 0 Human Binding pKd = 8.0 8.0 -3 5
Binding affinity to human muscarinic M4 receptor expressed in CHO-K9 cells incubated in dark at 22 degree C for 2 hrs by FACSCalibur flow cytometric saturation binding studyBinding affinity to human muscarinic M4 receptor expressed in CHO-K9 cells incubated in dark at 22 degree C for 2 hrs by FACSCalibur flow cytometric saturation binding study
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
10274019 204251 None 0 Human Binding pKi = 10.2 10.2 1 5
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 204251 None 0 Human Binding pKi = 10.2 10.2 1 5
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
71452756 79541 None 0 Human Binding pKi = 10.1 10.1 -2 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 79541 None 0 Human Binding pKi = 10.1 10.1 -2 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
49800047 14483 None 1 Human Binding pKi = 10.0 10.0 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14483 None 1 Human Binding pKi = 10.0 10.0 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14483 None 1 Human Binding pKi = 10.0 10.0 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
174174 523 None 49 Human Binding pKi = 10.0 10.0 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
174174.0 523 None 49 Human Binding pKi = 10.0 10.0 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
260 523 None 49 Human Binding pKi = 10.0 10.0 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
320 523 None 49 Human Binding pKi = 10.0 10.0 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 523 None 49 Human Binding pKi = 10.0 10.0 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 523 None 49 Human Binding pKi = 10.0 10.0 -2 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
16065403 67935 None 23 Human Binding pKi = 9.9 9.9 -1 5
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 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 67935 None 23 Human Binding pKi = 9.9 9.9 -1 5
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 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
23724781.0 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
CHEMBL1354199 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
23724781.0 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
CHEMBL1354199 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
23724781.0 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
316 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
CHEMBL1354199 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 2835 None 19 Human Binding pKi = 9.9 9.9 -9 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
2028 2979 None 80 Human Binding pKi = 9.6 9.6 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 2979 None 80 Human Binding pKi = 9.6 9.6 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 2979 None 80 Human Binding pKi = 9.6 9.6 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634.0 2979 None 80 Human Binding pKi = 9.6 9.6 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 2979 None 80 Human Binding pKi = 9.6 9.6 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 2979 None 80 Human Binding pKi = 9.6 9.6 -1 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
71454563 79656 None 0 Human Binding pKi = 9.5 9.5 -5 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 79656 None 0 Human Binding pKi = 9.5 9.5 -5 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
9867847 204258 None 0 Human Binding pKi = 9.5 9.5 -1 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 204258 None 0 Human Binding pKi = 9.5 9.5 -1 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
1201549 597 None 24 Human Binding pKi = 9.5 9.5 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
1201549.0 597 None 24 Human Binding pKi = 9.5 9.5 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
333 597 None 24 Human Binding pKi = 9.5 9.5 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 597 None 24 Human Binding pKi = 9.5 9.5 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 597 None 24 Human Binding pKi = 9.5 9.5 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 597 None 24 Human Binding pKi = 9.5 9.5 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 597 None 24 Human Binding pKi = 9.5 9.5 -1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
174174 523 None 49 Human Binding pKi = 9.5 9.5 -2 14
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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
174174.0 523 None 49 Human Binding pKi = 9.5 9.5 -2 14
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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
260 523 None 49 Human Binding pKi = 9.5 9.5 -2 14
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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
320 523 None 49 Human Binding pKi = 9.5 9.5 -2 14
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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 523 None 49 Human Binding pKi = 9.5 9.5 -2 14
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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 523 None 49 Human Binding pKi = 9.5 9.5 -2 14
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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
44610056 123991 None 0 Human Binding pKi = 9.5 9.5 -2 5
Antagonist activity at muscarinic M4 receptor (unknown origin)Antagonist activity at muscarinic M4 receptor (unknown origin)
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 123991 None 0 Human Binding pKi = 9.5 9.5 -2 5
Antagonist activity at muscarinic M4 receptor (unknown origin)Antagonist activity at muscarinic M4 receptor (unknown origin)
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
1734 116 None 10 Human Binding pKi = 9.4 9.4 -1 12
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 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 None 10 Human Binding pKi = 9.4 9.4 -1 12
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 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 None 10 Human Binding pKi = 9.4 9.4 -1 12
Binding affinity to human muscarinic M4 receptor by radioligand displacement assayBinding affinity to human muscarinic M4 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
25897919 55652 None 14 Human Binding pKi = 9.4 9.4 -3 8
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 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
657308.0 55652 None 14 Human Binding pKi = 9.4 9.4 -3 8
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 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 55652 None 14 Human Binding pKi = 9.4 9.4 -3 8
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 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 55652 None 14 Human Binding pKi = 9.4 9.4 -3 8
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 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 55652 None 14 Human Binding pKi = 9.4 9.4 -3 8
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 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
DB00332 55652 None 14 Human Binding pKi = 9.4 9.4 -3 8
Displacement of [3H]-NMS from human recombinant M4 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M4 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
3042 1414 None 35 Human Binding pKi = 9.4 9.4 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
3042.0 1414 None 35 Human Binding pKi = 9.4 9.4 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1414 None 35 Human Binding pKi = 9.4 9.4 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1414 None 35 Human Binding pKi = 9.4 9.4 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1414 None 35 Human Binding pKi = 9.4 9.4 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1414 None 35 Human Binding pKi = 9.4 9.4 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
162645520 183628 None 0 Human Binding pKi = 9.4 9.4 1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183628 None 0 Human Binding pKi = 9.4 9.4 1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183628 None 0 Human Binding pKi = 9.4 9.4 1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
156014450 178251 None 0 Human Binding pKi = 9.4 9.4 -2 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178251 None 0 Human Binding pKi = 9.4 9.4 -2 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178251 None 0 Human Binding pKi = 9.4 9.4 -2 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
16116083 12296 None 0 Human Binding pKi = 9.3 9.3 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 12296 None 0 Human Binding pKi = 9.3 9.3 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 12296 None 0 Human Binding pKi = 9.3 9.3 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
137630050 161040 None 0 Human Binding pKi = 9.3 9.3 -1 5
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 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 161040 None 0 Human Binding pKi = 9.3 9.3 -1 5
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 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 161040 None 0 Human Binding pKi = 9.3 9.3 -1 5
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 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 161040 None 0 Human Binding pKi = 9.3 9.3 -1 5
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 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
1734 116 None 10 Human Binding pKi = 9.3 9.3 -1 12
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
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 None 10 Human Binding pKi = 9.3 9.3 -1 12
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
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 None 10 Human Binding pKi = 9.3 9.3 -1 12
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
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 None 10 Rat Binding pKi = 9.3 9.3 -3 12
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell 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 None 10 Rat Binding pKi = 9.3 9.3 -3 12
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell 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 None 10 Rat Binding pKi = 9.3 9.3 -3 12
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell 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
174174 523 None 49 Rat Binding pKi = 9.3 9.3 1 14
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 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
174174.0 523 None 49 Rat Binding pKi = 9.3 9.3 1 14
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 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
260 523 None 49 Rat Binding pKi = 9.3 9.3 1 14
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 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
320 523 None 49 Rat Binding pKi = 9.3 9.3 1 14
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 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 523 None 49 Rat Binding pKi = 9.3 9.3 1 14
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 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 523 None 49 Rat Binding pKi = 9.3 9.3 1 14
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 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
CHEMBL5289601 194472 None 0 Human Binding pKi = 9.3 9.3 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 973 22 2 5 14.1 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
154417 93260 None 60 Rat Binding pKi = 9.3 9.3 -2 9
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 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
154417.0 93260 None 60 Rat Binding pKi = 9.3 9.3 -2 9
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 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
CHEMBL1331216 93260 None 60 Rat Binding pKi = 9.3 9.3 -2 9
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 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 93260 None 60 Rat Binding pKi = 9.3 9.3 -2 9
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 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
DB00424 93260 None 60 Rat Binding pKi = 9.3 9.3 -2 9
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 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
174174 523 None 49 Human Binding pKi = 9.2 9.2 -2 14
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
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.2017.05.042
174174.0 523 None 49 Human Binding pKi = 9.2 9.2 -2 14
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
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.2017.05.042
260 523 None 49 Human Binding pKi = 9.2 9.2 -2 14
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
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.2017.05.042
320 523 None 49 Human Binding pKi = 9.2 9.2 -2 14
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
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.2017.05.042
CHEMBL517712 523 None 49 Human Binding pKi = 9.2 9.2 -2 14
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
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.2017.05.042
DB00572 523 None 49 Human Binding pKi = 9.2 9.2 -2 14
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
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.2017.05.042
1734 116 None 10 Human Binding pKi = 9.2 9.2 -1 12
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
307 116 None 10 Human Binding pKi = 9.2 9.2 -1 12
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
CHEMBL168067 116 None 10 Human Binding pKi = 9.2 9.2 -1 12
Displacement of radiolabeled 4DAMP from human muscarinic M4 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M4 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
164611189 188471 None 0 Human Binding pKi = 9.2 9.2 -3 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 944 24 11 12 0.6 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4851514 188471 None 0 Human Binding pKi = 9.2 9.2 -3 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 944 24 11 12 0.6 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028061 188471 None 0 Human Binding pKi = 9.2 9.2 -3 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 944 24 11 12 0.6 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
46188794 178319 None 0 Human Binding pKi = 9.2 9.2 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178319 None 0 Human Binding pKi = 9.2 9.2 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178319 None 0 Human Binding pKi = 9.2 9.2 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
16115947 11849 None 0 Human Binding pKi = 9.2 9.2 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 11849 None 0 Human Binding pKi = 9.2 9.2 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 11849 None 0 Human Binding pKi = 9.2 9.2 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
164625454 188591 None 0 Human Binding pKi = 9.1 9.1 -3 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 1001 26 12 13 -0.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4862735 188591 None 0 Human Binding pKi = 9.1 9.1 -3 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 1001 26 12 13 -0.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028885 188591 None 0 Human Binding pKi = 9.1 9.1 -3 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 1001 26 12 13 -0.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
180 401 None 56 Human Binding pKi = 9.1 9.1 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 None 56 Human Binding pKi = 9.1 9.1 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 None 56 Human Binding pKi = 9.1 9.1 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160.0 401 None 56 Human Binding pKi = 9.1 9.1 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 None 56 Human Binding pKi = 9.1 9.1 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 None 56 Human Binding pKi = 9.1 9.1 -6 40
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
164612662 188482 None 0 Human Binding pKi = 9.1 9.1 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 845 20 8 11 0.9 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4847898 188482 None 0 Human Binding pKi = 9.1 9.1 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 845 20 8 11 0.9 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028154 188482 None 0 Human Binding pKi = 9.1 9.1 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 845 20 8 11 0.9 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
2745 3861 None 42 Human Binding pKi = 9.1 9.1 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572 3861 None 42 Human Binding pKi = 9.1 9.1 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572.0 3861 None 42 Human Binding pKi = 9.1 9.1 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
66007 3861 None 42 Human Binding pKi = 9.1 9.1 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
7315 3861 None 42 Human Binding pKi = 9.1 9.1 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
CHEMBL1490 3861 None 42 Human Binding pKi = 9.1 9.1 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
DB00376 3861 None 42 Human Binding pKi = 9.1 9.1 -5 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
9936450 35155 None 0 Human Binding pKi = 9.1 9.1 1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 35155 None 0 Human Binding pKi = 9.1 9.1 1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
164622681 188562 None 0 Human Binding pKi = 9.1 9.1 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4864727 188562 None 0 Human Binding pKi = 9.1 9.1 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028712 188562 None 0 Human Binding pKi = 9.1 9.1 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156014269 177216 None 0 Human Binding pKi = 9.1 9.1 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 177216 None 0 Human Binding pKi = 9.1 9.1 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
CHEMBL5289667 194475 None 0 Human Binding pKi = 9.1 9.1 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 959 21 2 5 13.8 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCCCN3CCC(OC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
CHEMBL5271406 193681 None 0 Human Binding pKi = 9.1 9.1 3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
16116085 11846 None 0 Human Binding pKi = 9.1 9.1 -8 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 11846 None 0 Human Binding pKi = 9.1 9.1 -8 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 11846 None 0 Human Binding pKi = 9.1 9.1 -8 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
16115945 12297 None 0 Human Binding pKi = 9.1 9.1 -4 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 12297 None 0 Human Binding pKi = 9.1 9.1 -4 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 12297 None 0 Human Binding pKi = 9.1 9.1 -4 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
1734 116 None 10 Human Binding pKi = 9.1 9.1 -1 12
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M4 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 None 10 Human Binding pKi = 9.1 9.1 -1 12
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M4 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 None 10 Human Binding pKi = 9.1 9.1 -1 12
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M4 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
118719922 115775 None 0 Human Binding pKi = 9.1 9.1 -1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115775 None 0 Human Binding pKi = 9.1 9.1 -1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
CHEMBL5273907 193785 None 0 Human Binding pKi = 9.1 9.1 2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 945 20 2 5 13.3 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
155521894 176425 None 0 Human Binding pKi = 9.0 9.0 -11 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176425 None 0 Human Binding pKi = 9.0 9.0 -11 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176425 None 0 Human Binding pKi = 9.0 9.0 -11 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
75167447 178286 None 0 Human Binding pKi = 9.0 9.0 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178286 None 0 Human Binding pKi = 9.0 9.0 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178286 None 0 Human Binding pKi = 9.0 9.0 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
162677523 183674 None 0 Human Binding pKi = 9.0 9.0 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183674 None 0 Human Binding pKi = 9.0 9.0 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183674 None 0 Human Binding pKi = 9.0 9.0 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
10160073 111189 None 0 Human Binding pKi = 9 9.0 151 5
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm301774u
CHEMBL326450 111189 None 0 Human Binding pKi = 9 9.0 151 5
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm301774u
16115797 138155 None 0 Human Binding pKi = 9 9.0 -2 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 138155 None 0 Human Binding pKi = 9 9.0 -2 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
10160219 4930 None 0 Human Binding pKi = 9 9.0 100 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 436 5 1 5 5.5 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL104693 4930 None 0 Human Binding pKi = 9 9.0 100 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 436 5 1 5 5.5 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
10160073 111189 None 0 Human Binding pKi = 9 9.0 151 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL326450 111189 None 0 Human Binding pKi = 9 9.0 151 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
2286 3183 None 51 Human Binding pKi = 9.0 9.0 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3183 None 51 Human Binding pKi = 9.0 9.0 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927.0 3183 None 51 Human Binding pKi = 9.0 9.0 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3183 None 51 Human Binding pKi = 9.0 9.0 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3183 None 51 Human Binding pKi = 9.0 9.0 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3183 None 51 Human Binding pKi = 9.0 9.0 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
155523648 176593 None 0 Human Binding pKi = 9.0 9.0 -7 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176593 None 0 Human Binding pKi = 9.0 9.0 -7 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176593 None 0 Human Binding pKi = 9.0 9.0 -7 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
101882890 115776 None 0 Human Binding pKi = 9.0 9.0 -1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115776 None 0 Human Binding pKi = 9.0 9.0 -1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
155550436 176501 None 0 Human Binding pKi = 9.0 9.0 -14 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176501 None 0 Human Binding pKi = 9.0 9.0 -14 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176501 None 0 Human Binding pKi = 9.0 9.0 -14 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
16115798 137878 None 0 Human Binding pKi = 8.9 8.9 1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 137878 None 0 Human Binding pKi = 8.9 8.9 1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
155560305 176253 None 0 Human Binding pKi = 8.9 8.9 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176253 None 0 Human Binding pKi = 8.9 8.9 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176253 None 0 Human Binding pKi = 8.9 8.9 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
16115799 83442 None 0 Human Binding pKi = 8.9 8.9 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 83442 None 0 Human Binding pKi = 8.9 8.9 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
155556290 176456 None 0 Human Binding pKi = 8.9 8.9 -7 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176456 None 0 Human Binding pKi = 8.9 8.9 -7 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176456 None 0 Human Binding pKi = 8.9 8.9 -7 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
174174 523 None 49 Human Binding pKi = 8.9 8.9 -2 14
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
174174.0 523 None 49 Human Binding pKi = 8.9 8.9 -2 14
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
260 523 None 49 Human Binding pKi = 8.9 8.9 -2 14
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
320 523 None 49 Human Binding pKi = 8.9 8.9 -2 14
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 523 None 49 Human Binding pKi = 8.9 8.9 -2 14
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 523 None 49 Human Binding pKi = 8.9 8.9 -2 14
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
CHEMBL5285607 194304 None 0 Human Binding pKi = 8.9 8.9 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
164614083 188491 None 0 Human Binding pKi = 8.8 8.8 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4855492 188491 None 0 Human Binding pKi = 8.8 8.8 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028231 188491 None 0 Human Binding pKi = 8.8 8.8 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164624066 188580 None 0 Human Binding pKi = 8.8 8.8 -6 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 787 18 7 10 1.8 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4864987 188580 None 0 Human Binding pKi = 8.8 8.8 -6 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 787 18 7 10 1.8 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028806 188580 None 0 Human Binding pKi = 8.8 8.8 -6 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 787 18 7 10 1.8 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
5284632 67402 None 13 Human Binding pKi = 8.8 8.8 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
5284632.0 67402 None 13 Human Binding pKi = 8.8 8.8 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 67402 None 13 Human Binding pKi = 8.8 8.8 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 67402 None 13 Human Binding pKi = 8.8 8.8 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
DB00209 67402 None 13 Human Binding pKi = 8.8 8.8 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
10628017 21716 None 0 Rat Binding pKi = 8.8 8.8 -3 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 650 26 3 7 7.0 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL131865 21716 None 0 Rat Binding pKi = 8.8 8.8 -3 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 650 26 3 7 7.0 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
57326235 77185 None 0 Human Binding pKi = 8.8 8.8 -2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77185 None 0 Human Binding pKi = 8.8 8.8 -2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77185 None 0 Human Binding pKi = 8.8 8.8 -2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
24846938 89801 None 0 Human Binding pKi = 8.8 8.8 -1 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 89801 None 0 Human Binding pKi = 8.8 8.8 -1 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
15157137 99895 None 0 Human Binding pKi = 8.8 8.8 1 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 317 7 0 3 4.0 CN(C)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL286008 99895 None 0 Human Binding pKi = 8.8 8.8 1 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 317 7 0 3 4.0 CN(C)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
302 2977 None 25 Human Binding pKi = 8.8 8.8 -7 8
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
4630 2977 None 25 Human Binding pKi = 8.8 8.8 -7 8
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
CHEMBL7634 2977 None 25 Human Binding pKi = 8.8 8.8 -7 8
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
174174 523 None 49 Human Binding pKi = 8.8 8.8 -2 14
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
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.2017.04.009
174174.0 523 None 49 Human Binding pKi = 8.8 8.8 -2 14
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
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.2017.04.009
260 523 None 49 Human Binding pKi = 8.8 8.8 -2 14
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
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.2017.04.009
320 523 None 49 Human Binding pKi = 8.8 8.8 -2 14
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
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.2017.04.009
CHEMBL517712 523 None 49 Human Binding pKi = 8.8 8.8 -2 14
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
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.2017.04.009
DB00572 523 None 49 Human Binding pKi = 8.8 8.8 -2 14
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
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.2017.04.009
155567380 176408 None 0 Human Binding pKi = 8.8 8.8 -20 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176408 None 0 Human Binding pKi = 8.8 8.8 -20 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176408 None 0 Human Binding pKi = 8.8 8.8 -20 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
CHEMBL5289083 194458 None 0 Human Binding pKi = 8.8 8.8 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1002 24 3 6 13.3 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCNCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
16115943 11847 None 0 Human Binding pKi = 8.7 8.7 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 11847 None 0 Human Binding pKi = 8.7 8.7 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 11847 None 0 Human Binding pKi = 8.7 8.7 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
164624669 188586 None 0 Human Binding pKi = 8.7 8.7 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4870127 188586 None 0 Human Binding pKi = 8.7 8.7 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028837 188586 None 0 Human Binding pKi = 8.7 8.7 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 674 15 6 8 2.1 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
16115796 137217 None 0 Human Binding pKi = 8.7 8.7 -2 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 137217 None 0 Human Binding pKi = 8.7 8.7 -2 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
9809330 115999 None 0 Human Binding pKi = 8.7 8.7 -18 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0301235
CHEMBL335542 115999 None 0 Human Binding pKi = 8.7 8.7 -18 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0301235
372625 101147 None 11 Human Binding pKi = 8.7 8.7 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 101147 None 11 Human Binding pKi = 8.7 8.7 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
155566290 176580 None 0 Human Binding pKi = 8.7 8.7 -25 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 176580 None 0 Human Binding pKi = 8.7 8.7 -25 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 176580 None 0 Human Binding pKi = 8.7 8.7 -25 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
372625 101147 None 11 Human Binding pKi = 8.7 8.7 -6 5
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in NG108-15 cells by scintillation counting analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in NG108-15 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 101147 None 11 Human Binding pKi = 8.7 8.7 -6 5
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in NG108-15 cells by scintillation counting analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in NG108-15 cells by scintillation counting analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1039/d0md00137f
10203251 5224 None 0 Human Binding pKi = 8.7 8.7 35 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 434 5 0 6 4.8 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(OC)cc2CCN1C3 10.1021/jm011116o
CHEMBL106224 5224 None 0 Human Binding pKi = 8.7 8.7 35 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 434 5 0 6 4.8 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(OC)cc2CCN1C3 10.1021/jm011116o
9911615 99031 None 0 Human Binding pKi = 8.7 8.7 114 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 450 5 0 6 5.5 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(SC)cc2CCN1C3 10.1021/jm011116o
CHEMBL280220 99031 None 0 Human Binding pKi = 8.7 8.7 114 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 450 5 0 6 5.5 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(SC)cc2CCN1C3 10.1021/jm011116o
9931930 108600 None 0 Human Binding pKi = 8.7 8.7 35 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 5 1 5 4.8 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL320465 108600 None 0 Human Binding pKi = 8.7 8.7 35 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 5 1 5 4.8 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
129989 451 None 51 Rat Binding pKi = 8 8.0 -2 9
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
8584 451 None 51 Rat Binding pKi = 8 8.0 -2 9
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
CHEMBL43383 451 None 51 Rat Binding pKi = 8 8.0 -2 9
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
119357 304 None 49 Human Binding pKi = 8 8.0 -1 6
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 304 None 49 Human Binding pKi = 8 8.0 -1 6
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
368 304 None 49 Human Binding pKi = 8 8.0 -1 6
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 304 None 49 Human Binding pKi = 8 8.0 -1 6
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
10125445 76028 None 0 Human Binding pKi = 8 8.0 -3 5
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205654 76028 None 0 Human Binding pKi = 8 8.0 -3 5
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
119357 304 None 49 Human Binding pKi = 8 8.0 -1 6
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 304 None 49 Human Binding pKi = 8 8.0 -1 6
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
368 304 None 49 Human Binding pKi = 8 8.0 -1 6
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 304 None 49 Human Binding pKi = 8 8.0 -1 6
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
137637944 155815 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
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 155815 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranesDisplacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
164623076 188567 None 0 Human Binding pKi = 8.0 8.0 -27 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188567 None 0 Human Binding pKi = 8.0 8.0 -27 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188567 None 0 Human Binding pKi = 8.0 8.0 -27 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
155559741 176287 None 0 Human Binding pKi = 8.0 8.0 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176287 None 0 Human Binding pKi = 8.0 8.0 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176287 None 0 Human Binding pKi = 8.0 8.0 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
324 1925 None 15 Human Binding pKi = 8.0 8.0 -1 9
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 1925 None 15 Human Binding pKi = 8.0 8.0 -1 9
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 1925 None 15 Human Binding pKi = 8.0 8.0 -1 9
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 1925 None 15 Human Binding pKi = 8.0 8.0 -1 9
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 1925 None 15 Human Binding pKi = 8.0 8.0 -1 9
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 1925 None 15 Human Binding pKi = 8.0 8.0 -1 9
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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
164619973 188541 None 0 Human Binding pKi = 8.0 8.0 -33 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188541 None 0 Human Binding pKi = 8.0 8.0 -33 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188541 None 0 Human Binding pKi = 8.0 8.0 -33 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
10114698 4833 None 0 Human Binding pKi = 8.0 8.0 41 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 448 7 1 5 5.5 CCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL104210 4833 None 0 Human Binding pKi = 8.0 8.0 41 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 448 7 1 5 5.5 CCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
135398737 958 None 93 Human Binding pKi = 7 7.0 -7 89
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398737.0 958 None 93 Human Binding pKi = 7 7.0 -7 89
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 958 None 93 Human Binding pKi = 7 7.0 -7 89
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 958 None 93 Human Binding pKi = 7 7.0 -7 89
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 958 None 93 Human Binding pKi = 7 7.0 -7 89
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 958 None 93 Human Binding pKi = 7 7.0 -7 89
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
145960827 161380 None 0 Human Binding pKi = 7 7.0 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161380 None 0 Human Binding pKi = 7 7.0 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
44299589 196397 None 0 Human Binding pKi = 6 6.0 -1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 196397 None 0 Human Binding pKi = 6 6.0 -1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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
135398745 2914 None 112 Human Binding pKi = 6 6.0 -32 65
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 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
135398745.0 2914 None 112 Human Binding pKi = 6 6.0 -32 65
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 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 2914 None 112 Human Binding pKi = 6 6.0 -32 65
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 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 2914 None 112 Human Binding pKi = 6 6.0 -32 65
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 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 2914 None 112 Human Binding pKi = 6 6.0 -32 65
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 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
2337 3256 None 77 Human Binding pKi = 6 6.0 -26 62
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
50 3256 None 77 Human Binding pKi = 6 6.0 -26 62
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
5002 3256 None 77 Human Binding pKi = 6 6.0 -26 62
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
5002.0 3256 None 77 Human Binding pKi = 6 6.0 -26 62
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
CHEMBL716 3256 None 77 Human Binding pKi = 6 6.0 -26 62
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
DB01224 3256 None 77 Human Binding pKi = 6 6.0 -26 62
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
11012653 120820 None 0 Human Binding pKi = 6 6.0 -6 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120820 None 0 Human Binding pKi = 6 6.0 -6 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
56593934 65695 None 0 Human Binding pKi = 5 5.0 -2630 8
Inhibition of human muscarinic M4 receptorInhibition of human muscarinic M4 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 65695 None 0 Human Binding pKi = 5 5.0 -2630 8
Inhibition of human muscarinic M4 receptorInhibition of human muscarinic M4 receptor
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
44448530 12335 None 0 Human Binding pKi = 4 4.0 -1 2
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12335 None 0 Human Binding pKi = 4 4.0 -1 2
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12335 None 0 Human Binding pKi = 4 4.0 -1 2
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
44593617 187431 None 0 Human Binding pKi = 6.0 6.0 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187431 None 0 Human Binding pKi = 6.0 6.0 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
123603 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
2684.0 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
584 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
DB00185 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
164614364 188495 None 0 Human Binding pKi = 5.0 5.0 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 733 15 9 10 -1.0 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4847458 188495 None 0 Human Binding pKi = 5.0 5.0 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 733 15 9 10 -1.0 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028248 188495 None 0 Human Binding pKi = 5.0 5.0 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 733 15 9 10 -1.0 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
2733619 11911 None 8 Human Binding pKi = 7.0 7.0 -3 5
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 11911 None 8 Human Binding pKi = 7.0 7.0 -3 5
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 11911 None 8 Human Binding pKi = 7.0 7.0 -3 5
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 11911 None 8 Human Binding pKi = 7.0 7.0 -3 5
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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
44627739 198372 None 0 Human Binding pKi = 7.0 7.0 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 198372 None 0 Human Binding pKi = 7.0 7.0 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 333 4 1 3 4.3 CN1CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
44593623 187880 None 0 Human Binding pKi = 7.0 7.0 -6 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187880 None 0 Human Binding pKi = 7.0 7.0 -6 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187880 None 0 Human Binding pKi = 7.0 7.0 -6 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
15050948 102817 None 0 Rat Binding pKi = 6.0 6.0 -1 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 513 7 3 7 1.8 NCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
CHEMBL305403 102817 None 0 Rat Binding pKi = 6.0 6.0 -1 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 513 7 3 7 1.8 NCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
164611347 188474 None 0 Human Binding pKi = 6.0 6.0 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4856090 188474 None 0 Human Binding pKi = 6.0 6.0 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028070 188474 None 0 Human Binding pKi = 6.0 6.0 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
2200 3131 None 46 Human Binding pKi = 7.0 7.0 -2 12
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
328 3131 None 46 Human Binding pKi = 7.0 7.0 -2 12
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
4848 3131 None 46 Human Binding pKi = 7.0 7.0 -2 12
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
4848.0 3131 None 46 Human Binding pKi = 7.0 7.0 -2 12
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
CHEMBL9967 3131 None 46 Human Binding pKi = 7.0 7.0 -2 12
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
DB00670 3131 None 46 Human Binding pKi = 7.0 7.0 -2 12
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
71575122 86213 None 0 Human Binding pKi = 5.0 5.0 -45 4
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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 86213 None 0 Human Binding pKi = 5.0 5.0 -45 4
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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
154734599 2503 None 12 Human Binding pKi = 7.0 7.0 -2 11
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
327 2503 None 12 Human Binding pKi = 7.0 7.0 -2 11
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
4108 2503 None 12 Human Binding pKi = 7.0 7.0 -2 11
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
CHEMBL27673 2503 None 12 Human Binding pKi = 7.0 7.0 -2 11
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
155559291 176659 None 0 Human Binding pKi = 6.0 6.0 -3 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 689 16 5 7 3.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4563530 176659 None 0 Human Binding pKi = 6.0 6.0 -3 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 689 16 5 7 3.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4598099 176659 None 0 Human Binding pKi = 6.0 6.0 -3 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 689 16 5 7 3.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
109035013 180475 None 1 Human Binding pKi = 5.0 5.0 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180475 None 1 Human Binding pKi = 5.0 5.0 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
11048067 5579 None 0 Human Binding pKi = 7.0 7.0 1 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5579 None 0 Human Binding pKi = 7.0 7.0 1 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
44437227 11878 None 0 Human Binding pKi = 6.0 6.0 3 2
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 194 3 0 4 0.9 Cc1cc(OCC#CCN(C)C)no1 10.1016/j.bmc.2007.09.003
CHEMBL1182447 11878 None 0 Human Binding pKi = 6.0 6.0 3 2
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 194 3 0 4 0.9 Cc1cc(OCC#CCN(C)C)no1 10.1016/j.bmc.2007.09.003
CHEMBL239017 11878 None 0 Human Binding pKi = 6.0 6.0 3 2
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 194 3 0 4 0.9 Cc1cc(OCC#CCN(C)C)no1 10.1016/j.bmc.2007.09.003
164611279 188473 None 0 Human Binding pKi = 6.0 6.0 -4 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4854472 188473 None 0 Human Binding pKi = 6.0 6.0 -4 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028067 188473 None 0 Human Binding pKi = 6.0 6.0 -4 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164623185 188570 None 0 Human Binding pKi = 6.0 6.0 1 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 407 4 3 5 1.5 NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4864101 188570 None 0 Human Binding pKi = 6.0 6.0 1 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 407 4 3 5 1.5 NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028743 188570 None 0 Human Binding pKi = 6.0 6.0 1 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 407 4 3 5 1.5 NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
66561967 74704 None 0 Human Binding pKi = 6.0 6.0 -1 7
Inhibition of M4 muscarinic receptorInhibition of M4 muscarinic receptor
ChEMBL 213 2 0 1 2.0 C1CC2CCC1N2CC12C3C4C5C3C1C5C42 10.1016/j.bmcl.2012.04.077
CHEMBL2030626 74704 None 0 Human Binding pKi = 6.0 6.0 -1 7
Inhibition of M4 muscarinic receptorInhibition of M4 muscarinic receptor
ChEMBL 213 2 0 1 2.0 C1CC2CCC1N2CC12C3C4C5C3C1C5C42 10.1016/j.bmcl.2012.04.077
11061341 78919 None 0 Human Binding pKi = 8.0 8.0 -23 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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 78919 None 0 Human Binding pKi = 8.0 8.0 -23 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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
100 3805 None 58 Human Binding pKi = 8.0 8.0 -14 55
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3805 None 58 Human Binding pKi = 8.0 8.0 -14 55
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3805 None 58 Human Binding pKi = 8.0 8.0 -14 55
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3805 None 58 Human Binding pKi = 8.0 8.0 -14 55
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3805 None 58 Human Binding pKi = 8.0 8.0 -14 55
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
16086063 80562 None 0 Human Binding pKi = 8.0 8.0 -57 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 80562 None 0 Human Binding pKi = 8.0 8.0 -57 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
12872437 12058 None 0 Human Binding pKi = 8.0 8.0 -9 5
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
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 12058 None 0 Human Binding pKi = 8.0 8.0 -9 5
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
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 12058 None 0 Human Binding pKi = 8.0 8.0 -9 5
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
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
3652 4097 None 79 Human Binding pKi = 8.0 8.0 -3 18
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 4097 None 79 Human Binding pKi = 8.0 8.0 -3 18
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 4097 None 79 Human Binding pKi = 8.0 8.0 -3 18
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
60809.0 4097 None 79 Human Binding pKi = 8.0 8.0 -3 18
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 4097 None 79 Human Binding pKi = 8.0 8.0 -3 18
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 4097 None 79 Human Binding pKi = 8.0 8.0 -3 18
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
132947 3864 None 9 Human Binding pKi = 7.9 7.9 -22 9
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 3864 None 9 Human Binding pKi = 7.9 7.9 -22 9
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 3864 None 9 Human Binding pKi = 7.9 7.9 -22 9
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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
145960466 161523 None 0 Human Binding pKi = 7.9 7.9 -2 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161523 None 0 Human Binding pKi = 7.9 7.9 -2 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
132947 3864 None 9 Rat Binding pKi = 7.9 7.9 -15 9
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 3864 None 9 Rat Binding pKi = 7.9 7.9 -15 9
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 3864 None 9 Rat Binding pKi = 7.9 7.9 -15 9
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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
132947 3864 None 9 Rat Binding pKi = 7.9 7.9 -15 9
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 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 10.1021/jm00075a032
361 3864 None 9 Rat Binding pKi = 7.9 7.9 -15 9
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 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 10.1021/jm00075a032
CHEMBL265256 3864 None 9 Rat Binding pKi = 7.9 7.9 -15 9
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 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 10.1021/jm00075a032
CHEMBL69452 203974 None 0 Human Binding pKi = 5.0 5.0 -2 5
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 331 6 1 5 2.7 CCO/C(O)=C1\CN2CC(CCC2COCc2ccccc2)C1=O 10.1021/jm020572p
44439406 91813 None 0 Human Binding pKi = 5.0 5.0 -1 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 422 8 0 4 5.9 CCCCSC1=CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL241283 91813 None 0 Human Binding pKi = 5.0 5.0 -1 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 422 8 0 4 5.9 CCCCSC1=CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
71457690 83798 None 0 Human Binding pKi = 6.0 6.0 1 5
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205817 83798 None 0 Human Binding pKi = 6.0 6.0 1 5
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
118719929 115783 None 0 Human Binding pKi = 7.0 7.0 1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115783 None 0 Human Binding pKi = 7.0 7.0 1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
44593627 193299 None 0 Human Binding pKi = 7.0 7.0 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 193299 None 0 Human Binding pKi = 7.0 7.0 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 193299 None 0 Human Binding pKi = 7.0 7.0 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
162353386 180980 None 0 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180980 None 0 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
57326237 77183 None 0 Human Binding pKi = 5.0 5.0 -2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77183 None 0 Human Binding pKi = 5.0 5.0 -2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77183 None 0 Human Binding pKi = 5.0 5.0 -2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
44448457 11913 None 0 Human Binding pKi = 5.0 5.0 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11913 None 0 Human Binding pKi = 5.0 5.0 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11913 None 0 Human Binding pKi = 5.0 5.0 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
44448419 12336 None 0 Human Binding pKi = 5.0 5.0 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12336 None 0 Human Binding pKi = 5.0 5.0 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12336 None 0 Human Binding pKi = 5.0 5.0 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
24865895 96005 None 0 Human Binding pKi = 4.9 4.9 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 96005 None 0 Human Binding pKi = 4.9 4.9 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 96005 None 0 Human Binding pKi = 4.9 4.9 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
44422692 11853 None 0 Human Binding pKi = 4.9 4.9 -9 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 11853 None 0 Human Binding pKi = 4.9 4.9 -9 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 11853 None 0 Human Binding pKi = 4.9 4.9 -9 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 96005 None 0 Human Binding pKi = 4.9 4.9 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 96005 None 0 Human Binding pKi = 4.9 4.9 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 96005 None 0 Human Binding pKi = 4.9 4.9 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 96005 None 0 Human Binding pKi = 4.9 4.9 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 96005 None 0 Human Binding pKi = 4.9 4.9 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 96005 None 0 Human Binding pKi = 4.9 4.9 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
3191 102858 None 97 Human Binding pKi = 6.9 6.9 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
3191.0 102858 None 97 Human Binding pKi = 6.9 6.9 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 102858 None 97 Human Binding pKi = 6.9 6.9 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
DB11742 102858 None 97 Human Binding pKi = 6.9 6.9 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
71575027 86223 None 0 Human Binding pKi = 4.9 4.9 -24 5
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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 86223 None 0 Human Binding pKi = 4.9 4.9 -24 5
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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
44448385 11910 None 0 Human Binding pKi = 5.9 5.9 2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11910 None 0 Human Binding pKi = 5.9 5.9 2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11910 None 0 Human Binding pKi = 5.9 5.9 2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
44448606 11918 None 0 Human Binding pKi = 5.9 5.9 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11918 None 0 Human Binding pKi = 5.9 5.9 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11918 None 0 Human Binding pKi = 5.9 5.9 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 310 6 2 3 2.6 OC(CCCN1CCNCC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
44593622 187796 None 0 Human Binding pKi = 5.9 5.9 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187796 None 0 Human Binding pKi = 5.9 5.9 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187796 None 0 Human Binding pKi = 5.9 5.9 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
156013536 178311 None 0 Human Binding pKi = 5.9 5.9 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178311 None 0 Human Binding pKi = 5.9 5.9 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178311 None 0 Human Binding pKi = 5.9 5.9 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
145961125 161546 None 0 Human Binding pKi = 5.9 5.9 -3 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161546 None 0 Human Binding pKi = 5.9 5.9 -3 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
162353384 181090 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181090 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
6726 1280 None 51 Human Binding pKi = 6.9 6.9 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
6726.0 1280 None 51 Human Binding pKi = 6.9 6.9 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1280 None 51 Human Binding pKi = 6.9 6.9 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1280 None 51 Human Binding pKi = 6.9 6.9 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1280 None 51 Human Binding pKi = 6.9 6.9 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1280 None 51 Human Binding pKi = 6.9 6.9 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
164613559 188486 None 0 Human Binding pKi = 7.9 7.9 -38 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188486 None 0 Human Binding pKi = 7.9 7.9 -38 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188486 None 0 Human Binding pKi = 7.9 7.9 -38 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
70685504 74454 None 0 Human Binding pKi = 7.9 7.9 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 74454 None 0 Human Binding pKi = 7.9 7.9 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 74454 None 0 Human Binding pKi = 7.9 7.9 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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
135398737 958 None 93 Human Binding pKi = 7.9 7.9 -7 89
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
135398737.0 958 None 93 Human Binding pKi = 7.9 7.9 -7 89
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
38 958 None 93 Human Binding pKi = 7.9 7.9 -7 89
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
722 958 None 93 Human Binding pKi = 7.9 7.9 -7 89
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL42 958 None 93 Human Binding pKi = 7.9 7.9 -7 89
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
DB00363 958 None 93 Human Binding pKi = 7.9 7.9 -7 89
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
135398745 2914 None 112 Human Binding pKi = 7.9 7.9 -32 65
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
135398745.0 2914 None 112 Human Binding pKi = 7.9 7.9 -32 65
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
47 2914 None 112 Human Binding pKi = 7.9 7.9 -32 65
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
CHEMBL715 2914 None 112 Human Binding pKi = 7.9 7.9 -32 65
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
DB00334 2914 None 112 Human Binding pKi = 7.9 7.9 -32 65
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
25067048 12333 None 0 Human Binding pKi = 7.9 7.9 28 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12333 None 0 Human Binding pKi = 7.9 7.9 28 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12333 None 0 Human Binding pKi = 7.9 7.9 28 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
16094788 141915 None 0 Human Binding pKi = 7.9 7.9 -5 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL386983 141915 None 0 Human Binding pKi = 7.9 7.9 -5 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
71449148 79538 None 0 Human Binding pKi = 7.9 7.9 -1 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 79538 None 0 Human Binding pKi = 7.9 7.9 -1 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
70687661 74453 None 0 Human Binding pKi = 7.9 7.9 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 74453 None 0 Human Binding pKi = 7.9 7.9 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 74453 None 0 Human Binding pKi = 7.9 7.9 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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
16086067 81317 None 0 Human Binding pKi = 6.9 6.9 -75 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 81317 None 0 Human Binding pKi = 6.9 6.9 -75 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
44439400 91214 None 0 Human Binding pKi = 4.9 4.9 -2 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 408 7 0 4 5.2 CCCOC1CCCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL240023 91214 None 0 Human Binding pKi = 4.9 4.9 -2 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 408 7 0 4 5.2 CCCOC1CCCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
44439391 145119 None 0 Human Binding pKi = 4.9 4.9 -331 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 336 3 2 4 3.3 COc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2007.01.093
CHEMBL391190 145119 None 0 Human Binding pKi = 4.9 4.9 -331 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 336 3 2 4 3.3 COc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2007.01.093
44274469 80608 None 1 Human Binding pKi = 4.9 4.9 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 80608 None 1 Human Binding pKi = 4.9 4.9 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
162649767 180102 None 0 Human Binding pKi = 4.9 4.9 -5 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 333 4 1 3 4.0 Cn1ccc2c(NC(=O)CCN3CCCc4ccccc43)cccc21 10.1016/j.bmcl.2020.127632
CHEMBL4748337 180102 None 0 Human Binding pKi = 4.9 4.9 -5 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 333 4 1 3 4.0 Cn1ccc2c(NC(=O)CCN3CCCc4ccccc43)cccc21 10.1016/j.bmcl.2020.127632
2733638 11914 None 2 Human Binding pKi = 6.9 6.9 -5 5
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 11914 None 2 Human Binding pKi = 6.9 6.9 -5 5
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 11914 None 2 Human Binding pKi = 6.9 6.9 -5 5
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 11914 None 2 Human Binding pKi = 6.9 6.9 -5 5
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 11914 None 2 Human Binding pKi = 6.9 6.9 -5 5
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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
9998508 80110 None 0 Human Binding pKi = 5.9 5.9 -2 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 80110 None 0 Human Binding pKi = 5.9 5.9 -2 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
11099206 120787 None 0 Human Binding pKi = 5.9 5.9 -3 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120787 None 0 Human Binding pKi = 5.9 5.9 -3 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
54816802 181272 None 2 Human Binding pKi = 5.9 5.9 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181272 None 2 Human Binding pKi = 5.9 5.9 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
44448500 12334 None 0 Human Binding pKi = 5.9 5.9 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12334 None 0 Human Binding pKi = 5.9 5.9 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12334 None 0 Human Binding pKi = 5.9 5.9 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
44274302 77067 None 0 Human Binding pKi = 4.9 4.9 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 77067 None 0 Human Binding pKi = 4.9 4.9 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
57326144 77191 None 0 Human Binding pKi = 4.9 4.9 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77191 None 0 Human Binding pKi = 4.9 4.9 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77191 None 0 Human Binding pKi = 4.9 4.9 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
71455894 83802 None 0 Human Binding pKi = 5.9 5.9 -1 12
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205827 83802 None 0 Human Binding pKi = 5.9 5.9 -1 12
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
71455894 83802 None 0 Human Binding pKi = 5.9 5.9 -1 12
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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 83802 None 0 Human Binding pKi = 5.9 5.9 -1 12
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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
2337 3256 None 77 Human Binding pKi = 6.9 6.9 -26 62
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
50 3256 None 77 Human Binding pKi = 6.9 6.9 -26 62
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
5002 3256 None 77 Human Binding pKi = 6.9 6.9 -26 62
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
5002.0 3256 None 77 Human Binding pKi = 6.9 6.9 -26 62
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
CHEMBL716 3256 None 77 Human Binding pKi = 6.9 6.9 -26 62
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
DB01224 3256 None 77 Human Binding pKi = 6.9 6.9 -26 62
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
164627253 188603 None 0 Human Binding pKi = 5.9 5.9 -28 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4876651 188603 None 0 Human Binding pKi = 5.9 5.9 -28 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028989 188603 None 0 Human Binding pKi = 5.9 5.9 -28 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44274441 99093 None 0 Human Binding pKi = 4.9 4.9 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 99093 None 0 Human Binding pKi = 4.9 4.9 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
73350931 92534 None 0 Human Binding pKi = 5.9 5.9 -2 5
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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 92534 None 0 Human Binding pKi = 5.9 5.9 -2 5
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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
73350823 102530 None 0 Human Binding pKi = 5.9 5.9 -83 9
Binding affinity to human muscarinic M4 receptor by competitive binding assayBinding affinity to human muscarinic M4 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2424668 102530 None 0 Human Binding pKi = 5.9 5.9 -83 9
Binding affinity to human muscarinic M4 receptor by competitive binding assayBinding affinity to human muscarinic M4 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 102530 None 0 Human Binding pKi = 5.9 5.9 -83 9
Binding affinity to human muscarinic M4 receptor by competitive binding assayBinding affinity to human muscarinic M4 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
11013666 59432 None 1 Human Binding pKi = 6.9 6.9 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 59432 None 1 Human Binding pKi = 6.9 6.9 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
154059 3637 None 51 Human Binding pKi = 6.9 6.9 -5 8
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
154059.0 3637 None 51 Human Binding pKi = 6.9 6.9 -5 8
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 3637 None 51 Human Binding pKi = 6.9 6.9 -5 8
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 3637 None 51 Human Binding pKi = 6.9 6.9 -5 8
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 3637 None 51 Human Binding pKi = 6.9 6.9 -5 8
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 3637 None 51 Human Binding pKi = 6.9 6.9 -5 8
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
137642607 158518 None 0 Human Binding pKi = 5.9 5.9 -660 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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 158518 None 0 Human Binding pKi = 5.9 5.9 -660 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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
162353388 180979 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180979 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
2398 954 None 62 Human Binding pKi = 7.9 7.9 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 954 None 62 Human Binding pKi = 7.9 7.9 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801.0 954 None 62 Human Binding pKi = 7.9 7.9 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 954 None 62 Human Binding pKi = 7.9 7.9 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 954 None 62 Human Binding pKi = 7.9 7.9 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 954 None 62 Human Binding pKi = 7.9 7.9 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
1971 2866 None 38 Human Binding pKi = 7.9 7.9 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2866 None 38 Human Binding pKi = 7.9 7.9 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2866 None 38 Human Binding pKi = 7.9 7.9 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543.0 2866 None 38 Human Binding pKi = 7.9 7.9 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2866 None 38 Human Binding pKi = 7.9 7.9 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2866 None 38 Human Binding pKi = 7.9 7.9 -3 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4134 72686 None 12 Human Binding pKi = 7.9 7.9 -8 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 72686 None 12 Human Binding pKi = 7.9 7.9 -8 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 72686 None 12 Human Binding pKi = 7.9 7.9 -8 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
164610746 188467 None 0 Human Binding pKi = 7.9 7.9 -34 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188467 None 0 Human Binding pKi = 7.9 7.9 -34 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188467 None 0 Human Binding pKi = 7.9 7.9 -34 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
2200 3131 None 46 Human Binding pKi = 7.9 7.9 -2 12
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 3131 None 46 Human Binding pKi = 7.9 7.9 -2 12
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 3131 None 46 Human Binding pKi = 7.9 7.9 -2 12
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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
4848.0 3131 None 46 Human Binding pKi = 7.9 7.9 -2 12
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 3131 None 46 Human Binding pKi = 7.9 7.9 -2 12
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 3131 None 46 Human Binding pKi = 7.9 7.9 -2 12
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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
10092649 193073 None 56 Human Binding pKi = 6.9 6.9 -11 9
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 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 193073 None 56 Human Binding pKi = 6.9 6.9 -11 9
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1021/jm100697g
611037 203694 None 1 Rat Binding pKi = 6.9 6.9 -2 4
Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M4 of NG108-15 cells.Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M4 of NG108-15 cells.
ChEMBL 399 4 1 5 2.2 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCl)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL67532 203694 None 1 Rat Binding pKi = 6.9 6.9 -2 4
Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M4 of NG108-15 cells.Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M4 of NG108-15 cells.
ChEMBL 399 4 1 5 2.2 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCl)CC2)c2ccccc21 10.1021/jm00111a032
71452387 83803 None 0 Human Binding pKi = 5.9 5.9 -1 7
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2012.08.046
CHEMBL2205829 83803 None 0 Human Binding pKi = 5.9 5.9 -1 7
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2012.08.046
71452387 83803 None 0 Human Binding pKi = 5.9 5.9 -1 7
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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 83803 None 0 Human Binding pKi = 5.9 5.9 -1 7
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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
73347826 92542 None 0 Human Binding pKi = 5.9 5.9 1 7
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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 92542 None 0 Human Binding pKi = 5.9 5.9 1 7
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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
CHEMBL5092747 215385 None 0 Human Binding pKi = 5.9 5.9 -6 5
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL None None None CC(=O)Nc1ccc(-c2cc(-c3ccccc3)nc3cc(C(=O)NCCCn4ccnc4)nn23)cc1 10.6019/CHEMBL5058647
CHEMBL5092747 215385 None 0 Human Binding pKi = 5.9 5.9 -6 5
GPCRScan assay: inhibition of M4GPCRScan assay: inhibition of M4
ChEMBL None None None CC(=O)Nc1ccc(-c2cc(-c3ccccc3)nc3cc(C(=O)NCCCn4ccnc4)nn23)cc1 10.6019/CHEMBL5058647
11001809 59081 None 0 Human Binding pKi = 4.9 4.9 -3 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 59081 None 0 Human Binding pKi = 4.9 4.9 -3 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
11112362 4959 None 0 Human Binding pKi = 5.9 5.9 -1 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 4959 None 0 Human Binding pKi = 5.9 5.9 -1 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
56672197 66562 None 0 Human Binding pKi = 5.9 5.9 2 3
Inhibition of M4 muscarinic receptor by NIMH PDSPInhibition of M4 muscarinic receptor by NIMH PDSP
ChEMBL 245 2 0 1 3.6 Fc1cccc(CN2C3CC4CC(C3)CC2C4)c1 10.1016/j.bmcl.2011.07.028
CHEMBL1824785 66562 None 0 Human Binding pKi = 5.9 5.9 2 3
Inhibition of M4 muscarinic receptor by NIMH PDSPInhibition of M4 muscarinic receptor by NIMH PDSP
ChEMBL 245 2 0 1 3.6 Fc1cccc(CN2C3CC4CC(C3)CC2C4)c1 10.1016/j.bmcl.2011.07.028
CHEMBL1852489 66562 None 0 Human Binding pKi = 5.9 5.9 2 3
Inhibition of M4 muscarinic receptor by NIMH PDSPInhibition of M4 muscarinic receptor by NIMH PDSP
ChEMBL 245 2 0 1 3.6 Fc1cccc(CN2C3CC4CC(C3)CC2C4)c1 10.1016/j.bmcl.2011.07.028
108993425 181758 None 1 Human Binding pKi = 5.9 5.9 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181758 None 1 Human Binding pKi = 5.9 5.9 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
24894637 188719 None 0 Human Binding pKi = 4.9 4.9 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 188719 None 0 Human Binding pKi = 4.9 4.9 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 188719 None 0 Human Binding pKi = 4.9 4.9 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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
11039424 78916 None 1 Human Binding pKi = 7.9 7.9 -45 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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 78916 None 1 Human Binding pKi = 7.9 7.9 -45 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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
5282593 55258 None 26 Human Binding pKi = 7.9 7.9 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 55258 None 26 Human Binding pKi = 7.9 7.9 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 55258 None 26 Human Binding pKi = 7.9 7.9 1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
44627740 198758 None 0 Human Binding pKi = 7.9 7.9 -11 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 198758 None 0 Human Binding pKi = 7.9 7.9 -11 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
10139614 5031 None 0 Human Binding pKi = 7.9 7.9 19 4
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 462 8 1 5 5.9 CCCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL105160 5031 None 0 Human Binding pKi = 7.9 7.9 19 4
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 462 8 1 5 5.9 CCCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
118719924 115778 None 0 Human Binding pKi = 7.8 7.8 2 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115778 None 0 Human Binding pKi = 7.8 7.8 2 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
9889312 78430 None 0 Human Binding pKi = 7.8 7.8 -2 5
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 78430 None 0 Human Binding pKi = 7.8 7.8 -2 5
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
3013846 188239 None 2 Human Binding pKi = 6.9 6.9 -1 5
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 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 188239 None 2 Human Binding pKi = 6.9 6.9 -1 5
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 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
11057 176149 None 23 Human Binding pKi = 6.9 6.9 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 176149 None 23 Human Binding pKi = 6.9 6.9 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 176149 None 23 Human Binding pKi = 6.9 6.9 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 176149 None 23 Human Binding pKi = 6.9 6.9 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
289 242 None 12 Human Binding pKi = 5.9 5.9 -128 14
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 242 None 12 Human Binding pKi = 5.9 5.9 -128 14
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 242 None 12 Human Binding pKi = 5.9 5.9 -128 14
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
44439396 91811 None 0 Human Binding pKi = 5.9 5.9 -7 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 348 3 0 3 4.3 CC(=O)OC1CCCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL241281 91811 None 0 Human Binding pKi = 5.9 5.9 -7 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 348 3 0 3 4.3 CC(=O)OC1CCCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
44318817 169114 None 0 Human Binding pKi = 5.9 5.9 -5 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL440138 169114 None 0 Human Binding pKi = 5.9 5.9 -5 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
9308 17754 None 21 Human Binding pKi = 5.9 5.9 -10 7
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
CHEMBL1255785 17754 None 21 Human Binding pKi = 5.9 5.9 -10 7
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
CHEMBL12587 17754 None 21 Human Binding pKi = 5.9 5.9 -10 7
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
CHEMBL292911 17754 None 21 Human Binding pKi = 5.9 5.9 -10 7
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
9308 17754 None 21 Rat Binding pKi = 5.9 5.9 -15 7
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
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 17754 None 21 Rat Binding pKi = 5.9 5.9 -15 7
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
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 17754 None 21 Rat Binding pKi = 5.9 5.9 -15 7
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
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 17754 None 21 Rat Binding pKi = 5.9 5.9 -15 7
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
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
1530 2182 None 50 Human Binding pKi = 6.9 6.9 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2182 None 50 Human Binding pKi = 6.9 6.9 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827.0 2182 None 50 Human Binding pKi = 6.9 6.9 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2182 None 50 Human Binding pKi = 6.9 6.9 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2182 None 50 Human Binding pKi = 6.9 6.9 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2182 None 50 Human Binding pKi = 6.9 6.9 -32 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
164619081 188537 None 0 Human Binding pKi = 6.9 6.9 -17 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4872720 188537 None 0 Human Binding pKi = 6.9 6.9 -17 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028531 188537 None 0 Human Binding pKi = 6.9 6.9 -17 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164621814 188556 None 0 Human Binding pKi = 6.9 6.9 -47 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4867301 188556 None 0 Human Binding pKi = 6.9 6.9 -47 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028667 188556 None 0 Human Binding pKi = 6.9 6.9 -47 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 718 18 8 9 1.9 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
145961495 161446 None 0 Human Binding pKi = 6.9 6.9 -2 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161446 None 0 Human Binding pKi = 6.9 6.9 -2 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
11120347 120729 None 0 Human Binding pKi = 5.9 5.9 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120729 None 0 Human Binding pKi = 5.9 5.9 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
162353391 180821 None 0 Human Binding pKi = 4.9 4.9 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180821 None 0 Human Binding pKi = 4.9 4.9 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
36381 12942 None 5 Human Binding pKi = 5.9 5.9 -4 6
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmcl.2012.08.046
CHEMBL1189234 12942 None 5 Human Binding pKi = 5.9 5.9 -4 6
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmcl.2012.08.046
36381 12942 None 5 Human Binding pKi = 5.9 5.9 -4 6
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmc.2013.07.045
CHEMBL1189234 12942 None 5 Human Binding pKi = 5.9 5.9 -4 6
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmc.2013.07.045
155521383 176426 None 0 Human Binding pKi = 6.8 6.8 -13 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176426 None 0 Human Binding pKi = 6.8 6.8 -13 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176426 None 0 Human Binding pKi = 6.8 6.8 -13 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
164621861 188557 None 0 Human Binding pKi = 5.8 5.8 -32 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4868124 188557 None 0 Human Binding pKi = 5.8 5.8 -32 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028673 188557 None 0 Human Binding pKi = 5.8 5.8 -32 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
639794 98769 None 1 Human Binding pKi = 4.8 4.8 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 98769 None 1 Human Binding pKi = 4.8 4.8 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
11809446 59679 None 0 Human Binding pKi = 4.8 4.8 -3 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 59679 None 0 Human Binding pKi = 4.8 4.8 -3 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
2683 102888 None 25 Human Binding pKi = 7.8 7.8 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102888 None 25 Human Binding pKi = 7.8 7.8 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102888 None 25 Human Binding pKi = 7.8 7.8 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
11004046 5454 None 0 Human Binding pKi = 7.8 7.8 33 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5454 None 0 Human Binding pKi = 7.8 7.8 33 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
11079969 163857 None 0 Human Binding pKi = 7.8 7.8 26 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 163857 None 0 Human Binding pKi = 7.8 7.8 26 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
71452793 79655 None 0 Human Binding pKi = 7.8 7.8 -1 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 79655 None 0 Human Binding pKi = 7.8 7.8 -1 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
10963509 18496 None 1 Human Binding pKi = 7.8 7.8 -1 5
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 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 18496 None 1 Human Binding pKi = 7.8 7.8 -1 5
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 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
44627746 14042 None 0 Human Binding pKi = 7.8 7.8 -7 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14042 None 0 Human Binding pKi = 7.8 7.8 -7 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14042 None 0 Human Binding pKi = 7.8 7.8 -7 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
164614388 188497 None 0 Human Binding pKi = 7.8 7.8 -6 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 23 12 11 0.1 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4848683 188497 None 0 Human Binding pKi = 7.8 7.8 -6 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 23 12 11 0.1 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028251 188497 None 0 Human Binding pKi = 7.8 7.8 -6 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 23 12 11 0.1 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
70681307 74456 None 0 Human Binding pKi = 7.8 7.8 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 74456 None 0 Human Binding pKi = 7.8 7.8 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 74456 None 0 Human Binding pKi = 7.8 7.8 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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
44593625 188130 None 0 Human Binding pKi = 7.8 7.8 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 188130 None 0 Human Binding pKi = 7.8 7.8 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 188130 None 0 Human Binding pKi = 7.8 7.8 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
14939893 9534 None 0 Rat Binding pKi = 7.8 7.8 -4 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL112244 9534 None 0 Rat Binding pKi = 7.8 7.8 -4 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
16086065 79797 None 0 Human Binding pKi = 6.8 6.8 -53 4
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 79797 None 0 Human Binding pKi = 6.8 6.8 -53 4
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
57326233 77186 None 0 Human Binding pKi = 6.8 6.8 -9 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77186 None 0 Human Binding pKi = 6.8 6.8 -9 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77186 None 0 Human Binding pKi = 6.8 6.8 -9 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
164626977 188599 None 0 Human Binding pKi = 5.8 5.8 -9 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 532 8 2 6 2.9 NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4874412 188599 None 0 Human Binding pKi = 5.8 5.8 -9 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 532 8 2 6 2.9 NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028969 188599 None 0 Human Binding pKi = 5.8 5.8 -9 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 532 8 2 6 2.9 NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44593621 193297 None 0 Human Binding pKi = 5.8 5.8 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 193297 None 0 Human Binding pKi = 5.8 5.8 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
118719928 115782 None 0 Human Binding pKi = 6.8 6.8 1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115782 None 0 Human Binding pKi = 6.8 6.8 1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
156010212 178237 None 0 Human Binding pKi = 6.8 6.8 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178237 None 0 Human Binding pKi = 6.8 6.8 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178237 None 0 Human Binding pKi = 6.8 6.8 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
46682613 181156 None 1 Human Binding pKi = 6.8 6.8 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181156 None 1 Human Binding pKi = 6.8 6.8 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
2726 919 None 68 Human Binding pKi = 6.8 6.8 -25 72
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
2726.0 919 None 68 Human Binding pKi = 6.8 6.8 -25 72
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
621 919 None 68 Human Binding pKi = 6.8 6.8 -25 72
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
83 919 None 68 Human Binding pKi = 6.8 6.8 -25 72
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
CHEMBL71 919 None 68 Human Binding pKi = 6.8 6.8 -25 72
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
DB00477 919 None 68 Human Binding pKi = 6.8 6.8 -25 72
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
44627741 197682 None 0 Human Binding pKi = 6.8 6.8 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 317 4 0 2 5.2 CN1CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL571123 197682 None 0 Human Binding pKi = 6.8 6.8 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 317 4 0 2 5.2 CN1CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
101720828 97120 None 0 Rat Binding pKi = 6.8 6.8 -16 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 97120 None 0 Rat Binding pKi = 6.8 6.8 -16 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 97120 None 0 Rat Binding pKi = 6.8 6.8 -16 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 97120 None 0 Rat Binding pKi = 6.8 6.8 -16 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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
10606253 157273 None 0 Rat Binding pKi = 6.8 6.8 -63 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 157273 None 0 Rat Binding pKi = 6.8 6.8 -63 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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
16094793 83322 None 0 Human Binding pKi = 6.8 6.8 -2 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
CHEMBL219118 83322 None 0 Human Binding pKi = 6.8 6.8 -2 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
16094810 137886 None 0 Human Binding pKi = 6.8 6.8 -1 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1 10.1021/jm0606995
CHEMBL376295 137886 None 0 Human Binding pKi = 6.8 6.8 -1 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1 10.1021/jm0606995
109013312 180134 None 1 Human Binding pKi = 5.8 5.8 -5 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180134 None 1 Human Binding pKi = 5.8 5.8 -5 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
162353375 179895 None 0 Human Binding pKi = 4.8 4.8 -4 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 179895 None 0 Human Binding pKi = 4.8 4.8 -4 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
156015141 178267 None 0 Human Binding pKi = 7.8 7.8 1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178267 None 0 Human Binding pKi = 7.8 7.8 1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178267 None 0 Human Binding pKi = 7.8 7.8 1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
10865439 20625 None 0 Human Binding pKi = 7.8 7.8 -1 5
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 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 20625 None 0 Human Binding pKi = 7.8 7.8 -1 5
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 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
302 2977 None 25 Human Binding pKi = 6.8 6.8 -7 8
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
4630 2977 None 25 Human Binding pKi = 6.8 6.8 -7 8
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
CHEMBL7634 2977 None 25 Human Binding pKi = 6.8 6.8 -7 8
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9904001
44439404 91785 None 0 Human Binding pKi = 5.8 5.8 -15 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 334 3 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL241103 91785 None 0 Human Binding pKi = 5.8 5.8 -15 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 334 3 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
1726 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993.0 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1726 2497 None 13 Human Binding pKi = 5.8 5.8 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 2497 None 13 Human Binding pKi = 5.8 5.8 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993.0 2497 None 13 Human Binding pKi = 5.8 5.8 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 2497 None 13 Human Binding pKi = 5.8 5.8 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 2497 None 13 Human Binding pKi = 5.8 5.8 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 2497 None 13 Human Binding pKi = 5.8 5.8 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
2812 4779 None 101 Human Binding pKi = 5.8 5.8 -19 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4779 None 101 Human Binding pKi = 5.8 5.8 -19 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
145960592 161361 None 0 Human Binding pKi = 6.8 6.8 -3 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161361 None 0 Human Binding pKi = 6.8 6.8 -3 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
122387447 138282 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 403 3 2 5 2.7 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1I 10.1039/C5MD00334B
CHEMBL3770686 138282 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 403 3 2 5 2.7 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1I 10.1039/C5MD00334B
137661377 159209 None 0 Human Binding pKi = 5.8 5.8 -316 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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 159209 None 0 Human Binding pKi = 5.8 5.8 -316 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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
107782 14468 None 18 Human Binding pKi = 5.8 5.8 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14468 None 18 Human Binding pKi = 5.8 5.8 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14468 None 18 Human Binding pKi = 5.8 5.8 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
71449073 78582 None 0 Rat Binding pKi = 5.8 5.8 -4 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 338 2 2 6 0.6 O=C1Nc2cccnc2N(C(=O)CN2CCNCC2)c2ncccc21 10.1021/jm00111a032
CHEMBL2112217 78582 None 0 Rat Binding pKi = 5.8 5.8 -4 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 338 2 2 6 0.6 O=C1Nc2cccnc2N(C(=O)CN2CCNCC2)c2ncccc21 10.1021/jm00111a032
44437298 11887 None 0 Human Binding pKi = 5.8 5.8 -7 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 11887 None 0 Human Binding pKi = 5.8 5.8 -7 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 11887 None 0 Human Binding pKi = 5.8 5.8 -7 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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
197842 102601 None 3 Human Binding pKi = 5.8 5.8 -56 3
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 102601 None 3 Human Binding pKi = 5.8 5.8 -56 3
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 102601 None 3 Human Binding pKi = 5.8 5.8 -56 3
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
10043954 82278 None 0 Human Binding pKi = 5.8 5.8 -5 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 82278 None 0 Human Binding pKi = 5.8 5.8 -5 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
10957754 59044 None 0 Human Binding pKi = 5.8 5.8 -6 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 59044 None 0 Human Binding pKi = 5.8 5.8 -6 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
162353369 180795 None 0 Human Binding pKi = 4.8 4.8 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180795 None 0 Human Binding pKi = 4.8 4.8 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
57326239 77182 None 0 Human Binding pKi = 4.8 4.8 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77182 None 0 Human Binding pKi = 4.8 4.8 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77182 None 0 Human Binding pKi = 4.8 4.8 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
4601 206747 None 35 Human Binding pKi = 7.8 7.8 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
4601.0 206747 None 35 Human Binding pKi = 7.8 7.8 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 206747 None 35 Human Binding pKi = 7.8 7.8 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 206747 None 35 Human Binding pKi = 7.8 7.8 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
DB01173 206747 None 35 Human Binding pKi = 7.8 7.8 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
155560140 176347 None 0 Human Binding pKi = 7.8 7.8 -11 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176347 None 0 Human Binding pKi = 7.8 7.8 -11 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176347 None 0 Human Binding pKi = 7.8 7.8 -11 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
5387 94879 None 31 Rat Binding pKi = 7.8 7.8 -22 5
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O 10.1021/jm00111a032
CHEMBL253978 94879 None 31 Rat Binding pKi = 7.8 7.8 -22 5
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O 10.1021/jm00111a032
71461681 79540 None 0 Human Binding pKi = 7.8 7.8 -5 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 79540 None 0 Human Binding pKi = 7.8 7.8 -5 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
122387447 138282 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 403 3 2 5 2.7 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1I 10.1039/C5MD00334B
CHEMBL3770686 138282 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 403 3 2 5 2.7 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1I 10.1039/C5MD00334B
15157141 92801 None 0 Human Binding pKi = 6.8 6.8 1 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 373 11 0 3 5.6 CCN(CC)CCCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL24369 92801 None 0 Human Binding pKi = 6.8 6.8 1 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 373 11 0 3 5.6 CCN(CC)CCCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
10360219 102010 None 0 Human Binding pKi = 6.8 6.8 -1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 102010 None 0 Human Binding pKi = 6.8 6.8 -1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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
132712 171798 None 19 Human Binding pKi = 6.8 6.8 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 171798 None 19 Human Binding pKi = 6.8 6.8 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
10595006 11445 None 0 Human Binding pKi = 5.8 5.8 -10 5
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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 11445 None 0 Human Binding pKi = 5.8 5.8 -10 5
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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 11445 None 0 Human Binding pKi = 5.8 5.8 -10 5
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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
44299635 100569 None 0 Human Binding pKi = 5.8 5.8 -1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 100569 None 0 Human Binding pKi = 5.8 5.8 -1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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
162353390 180949 None 0 Human Binding pKi = 5.8 5.8 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180949 None 0 Human Binding pKi = 5.8 5.8 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
155519621 170389 None 0 Human Binding pKi = 5.8 5.8 -54 4
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 90 mins by scintillation counting method
ChEMBL 345 2 2 6 2.7 Clc1ccc(C#Cc2nc(N[C@@H]3CCOC3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
CHEMBL4447908 170389 None 0 Human Binding pKi = 5.8 5.8 -54 4
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 90 mins by scintillation counting method
ChEMBL 345 2 2 6 2.7 Clc1ccc(C#Cc2nc(N[C@@H]3CCOC3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
145960427 161450 None 0 Human Binding pKi = 6.8 6.8 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161450 None 0 Human Binding pKi = 6.8 6.8 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
10066369 120258 None 0 Human Binding pKi = 5.8 5.8 -22 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120258 None 0 Human Binding pKi = 5.8 5.8 -22 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
162658421 181101 None 0 Human Binding pKi = 4.8 4.8 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181101 None 0 Human Binding pKi = 4.8 4.8 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
12739458 66551 None 0 Human Binding pKi = 5.8 5.8 2 3
Inhibition of M4 muscarinic receptor by NIMH PDSPInhibition of M4 muscarinic receptor by NIMH PDSP
ChEMBL 227 2 0 1 3.5 c1ccc(CN2C3CC4CC(C3)CC2C4)cc1 10.1016/j.bmcl.2011.07.028
CHEMBL1824784 66551 None 0 Human Binding pKi = 5.8 5.8 2 3
Inhibition of M4 muscarinic receptor by NIMH PDSPInhibition of M4 muscarinic receptor by NIMH PDSP
ChEMBL 227 2 0 1 3.5 c1ccc(CN2C3CC4CC(C3)CC2C4)cc1 10.1016/j.bmcl.2011.07.028
CHEMBL1852447 66551 None 0 Human Binding pKi = 5.8 5.8 2 3
Inhibition of M4 muscarinic receptor by NIMH PDSPInhibition of M4 muscarinic receptor by NIMH PDSP
ChEMBL 227 2 0 1 3.5 c1ccc(CN2C3CC4CC(C3)CC2C4)cc1 10.1016/j.bmcl.2011.07.028
71459971 79539 None 0 Human Binding pKi = 7.7 7.7 -1 3
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
CHEMBL2114066 79539 None 0 Human Binding pKi = 7.7 7.7 -1 3
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
214124 169691 None 2 Human Binding pKi = 7.7 7.7 -4 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 331 8 0 3 4.4 CCN(CC)CCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL443780 169691 None 2 Human Binding pKi = 7.7 7.7 -4 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 331 8 0 3 4.4 CCN(CC)CCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
10204457 204403 None 0 Human Binding pKi = 7.7 7.7 -2 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 204403 None 0 Human Binding pKi = 7.7 7.7 -2 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
164625419 188590 None 0 Human Binding pKi = 7.7 7.7 -5 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 504 8 2 6 3.0 NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4862087 188590 None 0 Human Binding pKi = 7.7 7.7 -5 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 504 8 2 6 3.0 NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028881 188590 None 0 Human Binding pKi = 7.7 7.7 -5 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 504 8 2 6 3.0 NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156015254 178287 None 0 Human Binding pKi = 7.7 7.7 -4 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178287 None 0 Human Binding pKi = 7.7 7.7 -4 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178287 None 0 Human Binding pKi = 7.7 7.7 -4 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
70683405 74475 None 0 Human Binding pKi = 7.7 7.7 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 74475 None 0 Human Binding pKi = 7.7 7.7 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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 74475 None 0 Human Binding pKi = 7.7 7.7 -3 4
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 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
44415886 79835 None 0 Human Binding pKi = 6.8 6.8 -74 4
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 79835 None 0 Human Binding pKi = 6.8 6.8 -74 4
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
44439390 147804 None 0 Human Binding pKi = 4.8 4.8 -398 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 322 4 2 3 3.6 COc1cccc(CC2NCCc3c2[nH]c2ccc(OC)cc32)c1 10.1016/j.bmcl.2007.01.093
CHEMBL393275 147804 None 0 Human Binding pKi = 4.8 4.8 -398 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 322 4 2 3 3.6 COc1cccc(CC2NCCc3c2[nH]c2ccc(OC)cc32)c1 10.1016/j.bmcl.2007.01.093
10066972 98754 None 0 Human Binding pKi = 5.7 5.7 -5 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 98754 None 0 Human Binding pKi = 5.7 5.7 -5 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
109035056 181323 None 1 Human Binding pKi = 4.7 4.7 -29 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 331 4 1 3 4.0 O=C(CCN1CCCc2ccccc21)Nc1cccc2cccnc12 10.1016/j.bmcl.2020.127632
CHEMBL4762755 181323 None 1 Human Binding pKi = 4.7 4.7 -29 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 331 4 1 3 4.0 O=C(CCN1CCCc2ccccc21)Nc1cccc2cccnc12 10.1016/j.bmcl.2020.127632
162353378 182911 None 0 Human Binding pKi = 4.7 4.7 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 182911 None 0 Human Binding pKi = 4.7 4.7 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
71575447 86202 None 0 Human Binding pKi = 5.7 5.7 -31 5
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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 86202 None 0 Human Binding pKi = 5.7 5.7 -31 5
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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
6075 150108 None 42 Human Binding pKi = 7.7 7.7 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150108 None 42 Human Binding pKi = 7.7 7.7 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
44593626 187853 None 0 Human Binding pKi = 7.7 7.7 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187853 None 0 Human Binding pKi = 7.7 7.7 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187853 None 0 Human Binding pKi = 7.7 7.7 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
44627852 14039 None 0 Human Binding pKi = 7.7 7.7 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14039 None 0 Human Binding pKi = 7.7 7.7 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14039 None 0 Human Binding pKi = 7.7 7.7 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
11071537 26496 None 0 Human Binding pKi = 7.7 7.7 -1 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 495 17 0 10 5.5 COc1nsnc1OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL136027 26496 None 0 Human Binding pKi = 7.7 7.7 -1 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 495 17 0 10 5.5 COc1nsnc1OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
164609510 188465 None 0 Human Binding pKi = 7.7 7.7 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 817 21 11 10 0.5 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4846562 188465 None 0 Human Binding pKi = 7.7 7.7 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 817 21 11 10 0.5 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5027965 188465 None 0 Human Binding pKi = 7.7 7.7 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 817 21 11 10 0.5 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
10651844 115489 None 0 Rat Binding pKi = 7.7 7.7 -2 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 649 22 3 7 5.2 CN(CCCCCCCCN(C)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
CHEMBL335115 115489 None 0 Rat Binding pKi = 7.7 7.7 -2 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 649 22 3 7 5.2 CN(CCCCCCCCN(C)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
2274 3173 None 58 Human Binding pKi = 6.7 6.7 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 None 58 Human Binding pKi = 6.7 6.7 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917.0 3173 None 58 Human Binding pKi = 6.7 6.7 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 None 58 Human Binding pKi = 6.7 6.7 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 None 58 Human Binding pKi = 6.7 6.7 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 None 58 Human Binding pKi = 6.7 6.7 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
10105296 205922 None 0 Human Binding pKi = 6.7 6.7 1 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
CHEMBL84113 205922 None 0 Human Binding pKi = 6.7 6.7 1 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
10982070 5166 None 0 Human Binding pKi = 6.7 6.7 2 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5166 None 0 Human Binding pKi = 6.7 6.7 2 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
44439410 147289 None 0 Human Binding pKi = 4.7 4.7 -5 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 280 4 1 2 3.5 CN(/C=N/c1ccc2c(c1)C(O)CC2)Cc1ccccc1 10.1016/j.bmcl.2007.01.093
CHEMBL392888 147289 None 0 Human Binding pKi = 4.7 4.7 -5 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 280 4 1 2 3.5 CN(/C=N/c1ccc2c(c1)C(O)CC2)Cc1ccccc1 10.1016/j.bmcl.2007.01.093
11759379 120777 None 0 Human Binding pKi = 5.7 5.7 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120777 None 0 Human Binding pKi = 5.7 5.7 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
441383 20333 None 57 Human Binding pKi = 5.7 5.7 -5 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 20333 None 57 Human Binding pKi = 5.7 5.7 -5 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
57664418 138300 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 325 4 2 5 3.1 CCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
CHEMBL3770870 138300 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 325 4 2 5 3.1 CCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
44299599 167805 None 0 Human Binding pKi = 5.7 5.7 -1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 167805 None 0 Human Binding pKi = 5.7 5.7 -1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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
164621085 188549 None 0 Human Binding pKi = 5.7 5.7 -18 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 830 17 8 11 -0.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4869980 188549 None 0 Human Binding pKi = 5.7 5.7 -18 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 830 17 8 11 -0.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028630 188549 None 0 Human Binding pKi = 5.7 5.7 -18 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 830 17 8 11 -0.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
10916286 5102 None 0 Human Binding pKi = 5.7 5.7 1 4
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5102 None 0 Human Binding pKi = 5.7 5.7 1 4
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(Cl)c2C1O3 10.1021/jm011116o
156015895 178281 None 0 Human Binding pKi = 6.7 6.7 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178281 None 0 Human Binding pKi = 6.7 6.7 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178281 None 0 Human Binding pKi = 6.7 6.7 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
137655636 158736 None 0 Human Binding pKi = 6.7 6.7 -93 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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 158736 None 0 Human Binding pKi = 6.7 6.7 -93 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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
11024241 120301 None 0 Human Binding pKi = 5.7 5.7 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120301 None 0 Human Binding pKi = 5.7 5.7 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
156011112 178275 None 0 Human Binding pKi = 5.7 5.7 -10 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178275 None 0 Human Binding pKi = 5.7 5.7 -10 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178275 None 0 Human Binding pKi = 5.7 5.7 -10 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
156015809 178318 None 0 Human Binding pKi = 5.7 5.7 -10 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178318 None 0 Human Binding pKi = 5.7 5.7 -10 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178318 None 0 Human Binding pKi = 5.7 5.7 -10 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
164612852 188483 None 0 Human Binding pKi = 4.7 4.7 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4852544 188483 None 0 Human Binding pKi = 4.7 4.7 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028161 188483 None 0 Human Binding pKi = 4.7 4.7 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
164622945 188565 None 0 Human Binding pKi = 8.7 8.7 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 646 14 6 7 3.6 N=C(N)NCCC[C@@H](NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)O 10.1016/j.ejmech.2021.113159
CHEMBL4871700 188565 None 0 Human Binding pKi = 8.7 8.7 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 646 14 6 7 3.6 N=C(N)NCCC[C@@H](NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)O 10.1016/j.ejmech.2021.113159
CHEMBL5028723 188565 None 0 Human Binding pKi = 8.7 8.7 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 646 14 6 7 3.6 N=C(N)NCCC[C@@H](NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)O 10.1016/j.ejmech.2021.113159
155550632 176529 None 0 Human Binding pKi = 8.7 8.7 -32 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176529 None 0 Human Binding pKi = 8.7 8.7 -32 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176529 None 0 Human Binding pKi = 8.7 8.7 -32 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
155566290 176580 None 0 Human Binding pKi = 8.7 8.7 -25 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176580 None 0 Human Binding pKi = 8.7 8.7 -25 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176580 None 0 Human Binding pKi = 8.7 8.7 -25 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
156015807 178299 None 0 Human Binding pKi = 8.7 8.7 -3 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178299 None 0 Human Binding pKi = 8.7 8.7 -3 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178299 None 0 Human Binding pKi = 8.7 8.7 -3 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
277 1301 None 62 Human Binding pKi = 8.7 8.7 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1301 None 62 Human Binding pKi = 8.7 8.7 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913.0 1301 None 62 Human Binding pKi = 8.7 8.7 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1301 None 62 Human Binding pKi = 8.7 8.7 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1301 None 62 Human Binding pKi = 8.7 8.7 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1301 None 62 Human Binding pKi = 8.7 8.7 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
10180872 103129 None 0 Human Binding pKi = 8.7 8.7 -2 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 103129 None 0 Human Binding pKi = 8.7 8.7 -2 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
155541812 173050 None 0 Human Binding pKi = 8.7 8.7 -1 5
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M4 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 173050 None 0 Human Binding pKi = 8.7 8.7 -1 5
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M4 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
10919522 78918 None 0 Human Binding pKi = 8.6 8.6 -9 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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 78918 None 0 Human Binding pKi = 8.6 8.6 -9 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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
16115951 141643 None 0 Human Binding pKi = 8.6 8.6 -2 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 141643 None 0 Human Binding pKi = 8.6 8.6 -2 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
57326326 77178 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77178 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77178 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
57326326 77178 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 77178 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 77178 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
156020548 178178 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178178 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
155554568 176609 None 0 Human Binding pKi = 8.6 8.6 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176609 None 0 Human Binding pKi = 8.6 8.6 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176609 None 0 Human Binding pKi = 8.6 8.6 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
9913341 82158 None 4 Human Binding pKi = 8.6 8.6 3 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL216927 82158 None 4 Human Binding pKi = 8.6 8.6 3 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL553058 82158 None 4 Human Binding pKi = 8.6 8.6 3 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
122203596 155806 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 155806 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 155806 None 0 Human Binding pKi = 8.6 8.6 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
164627113 188602 None 0 Human Binding pKi = 8.6 8.6 -13 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 489 7 2 5 4.2 NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4878646 188602 None 0 Human Binding pKi = 8.6 8.6 -13 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 489 7 2 5 4.2 NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028981 188602 None 0 Human Binding pKi = 8.6 8.6 -13 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 489 7 2 5 4.2 NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
9913341 82158 None 4 Human Binding pKi = 8.6 8.6 3 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 82158 None 4 Human Binding pKi = 8.6 8.6 3 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL553058 82158 None 4 Human Binding pKi = 8.6 8.6 3 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
155525097 170950 None 0 Human Binding pKi = 8.6 8.6 -32 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 170950 None 0 Human Binding pKi = 8.6 8.6 -32 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
156015900 178321 None 0 Human Binding pKi = 8.6 8.6 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178321 None 0 Human Binding pKi = 8.6 8.6 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178321 None 0 Human Binding pKi = 8.6 8.6 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
CHEMBL5268503 193567 None 0 Human Binding pKi = 8.6 8.6 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1038 20 1 13 9.7 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
42596929 77188 None 0 Human Binding pKi = 8.6 8.6 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77188 None 0 Human Binding pKi = 8.6 8.6 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77188 None 0 Human Binding pKi = 8.6 8.6 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
162645430 183627 None 0 Human Binding pKi = 8.6 8.6 1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183627 None 0 Human Binding pKi = 8.6 8.6 1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183627 None 0 Human Binding pKi = 8.6 8.6 1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
164615275 188507 None 0 Human Binding pKi = 8.6 8.6 -17 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 859 20 9 11 1.5 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4861252 188507 None 0 Human Binding pKi = 8.6 8.6 -17 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 859 20 9 11 1.5 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028304 188507 None 0 Human Binding pKi = 8.6 8.6 -17 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 859 20 9 11 1.5 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
155535606 172052 None 0 Human Binding pKi = 8.6 8.6 -7 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 172052 None 0 Human Binding pKi = 8.6 8.6 -7 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
162649253 183645 None 0 Human Binding pKi = 8.6 8.6 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183645 None 0 Human Binding pKi = 8.6 8.6 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183645 None 0 Human Binding pKi = 8.6 8.6 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
26987 949 None 33 Human Binding pKi = 8.6 8.6 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
26987.0 949 None 33 Human Binding pKi = 8.6 8.6 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 949 None 33 Human Binding pKi = 8.6 8.6 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 949 None 33 Human Binding pKi = 8.6 8.6 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 949 None 33 Human Binding pKi = 8.6 8.6 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 949 None 33 Human Binding pKi = 8.6 8.6 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
10771937 21693 None 0 Rat Binding pKi = 8.6 8.6 -5 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL1202004 21693 None 0 Rat Binding pKi = 8.6 8.6 -5 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL131846 21693 None 0 Rat Binding pKi = 8.6 8.6 -5 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
164628352 188613 None 0 Human Binding pKi = 8.5 8.5 -9 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 630 13 5 6 4.0 N=C(N)NCCCCC(=O)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4878717 188613 None 0 Human Binding pKi = 8.5 8.5 -9 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 630 13 5 6 4.0 N=C(N)NCCCCC(=O)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5029051 188613 None 0 Human Binding pKi = 8.5 8.5 -9 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 630 13 5 6 4.0 N=C(N)NCCCCC(=O)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156015978 178323 None 0 Human Binding pKi = 8.5 8.5 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178323 None 0 Human Binding pKi = 8.5 8.5 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178323 None 0 Human Binding pKi = 8.5 8.5 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
16086001 139214 None 0 Human Binding pKi = 7.7 7.7 -117 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 139214 None 0 Human Binding pKi = 7.7 7.7 -117 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
44439398 91213 None 0 Human Binding pKi = 6.7 6.7 1 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 408 5 0 5 4.4 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CCC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL240022 91213 None 0 Human Binding pKi = 6.7 6.7 1 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 408 5 0 5 4.4 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CCC3)CC2 10.1016/j.bmcl.2007.01.093
44439403 91784 None 0 Human Binding pKi = 6.7 6.7 5 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 394 5 0 5 4.0 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL241102 91784 None 0 Human Binding pKi = 6.7 6.7 5 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 394 5 0 5 4.0 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CC3)CC2 10.1016/j.bmcl.2007.01.093
44439399 147392 None 0 Human Binding pKi = 6.7 6.7 2 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 422 5 0 5 4.8 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CCCC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL392970 147392 None 0 Human Binding pKi = 6.7 6.7 2 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 422 5 0 5 4.8 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CCCC3)CC2 10.1016/j.bmcl.2007.01.093
57664418 138300 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 325 4 2 5 3.1 CCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
CHEMBL3770870 138300 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 325 4 2 5 3.1 CCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
44439401 91783 None 0 Human Binding pKi = 5.7 5.7 7 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 395 4 0 5 3.6 COC(=O)N1CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL241101 91783 None 0 Human Binding pKi = 5.7 5.7 7 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 395 4 0 5 3.6 COC(=O)N1CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
156308 169283 None 5 Human Binding pKi = 5.7 5.7 2 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 354 2 0 4 3.2 COc1ccc2c(c1OC)C[N+]1(C)CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmcl.2007.01.093
CHEMBL441356 169283 None 5 Human Binding pKi = 5.7 5.7 2 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 354 2 0 4 3.2 COc1ccc2c(c1OC)C[N+]1(C)CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmcl.2007.01.093
155551903 176457 None 0 Human Binding pKi = 6.7 6.7 -2 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176457 None 0 Human Binding pKi = 6.7 6.7 -2 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176457 None 0 Human Binding pKi = 6.7 6.7 -2 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
10236758 115772 None 5 Human Binding pKi = 6.7 6.7 -213 13
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115772 None 5 Human Binding pKi = 6.7 6.7 -213 13
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
44593623 187880 None 0 Human Binding pKi = 6.7 6.7 -6 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187880 None 0 Human Binding pKi = 6.7 6.7 -6 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187880 None 0 Human Binding pKi = 6.7 6.7 -6 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
92218234 120827 None 1 Human Binding pKi = 4.7 4.7 -12 4
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 120827 None 1 Human Binding pKi = 4.7 4.7 -12 4
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 120827 None 1 Human Binding pKi = 4.7 4.7 -12 4
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
15157140 99874 None 0 Human Binding pKi = 6.7 6.7 -1 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 359 10 0 3 5.2 CCN(CC)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL285898 99874 None 0 Human Binding pKi = 6.7 6.7 -1 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 359 10 0 3 5.2 CCN(CC)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
44568347 191651 None 0 Human Binding pKi = 7.7 7.7 3 15
Antagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M4 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 191651 None 0 Human Binding pKi = 7.7 7.7 3 15
Antagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M4 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
2726 919 None 68 Human Binding pKi = 7.7 7.7 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
2726.0 919 None 68 Human Binding pKi = 7.7 7.7 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 None 68 Human Binding pKi = 7.7 7.7 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 None 68 Human Binding pKi = 7.7 7.7 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 None 68 Human Binding pKi = 7.7 7.7 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 None 68 Human Binding pKi = 7.7 7.7 -25 72
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
15050955 102598 None 0 Rat Binding pKi = 6.7 6.7 -2 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 538 7 1 7 3.0 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCCN3C(=O)c4ccccc4C3=O)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL304112 102598 None 0 Rat Binding pKi = 6.7 6.7 -2 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 538 7 1 7 3.0 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCCN3C(=O)c4ccccc4C3=O)CC2)c2ccccc21 10.1021/jm00111a032
36014865 182670 None 2 Human Binding pKi = 6.7 6.7 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 182670 None 2 Human Binding pKi = 6.7 6.7 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
164608958 188460 None 0 Human Binding pKi = 5.7 5.7 -11 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4846447 188460 None 0 Human Binding pKi = 5.7 5.7 -11 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5027936 188460 None 0 Human Binding pKi = 5.7 5.7 -11 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCCNC(=N)N)NCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
162675053 183258 None 0 Human Binding pKi = 5.7 5.7 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 183258 None 0 Human Binding pKi = 5.7 5.7 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
44274400 98938 None 0 Human Binding pKi = 4.7 4.7 1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 98938 None 0 Human Binding pKi = 4.7 4.7 1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
162667844 182533 None 0 Human Binding pKi = 4.7 4.7 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 182533 None 0 Human Binding pKi = 4.7 4.7 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
24894625 9778 None 0 Human Binding pKi = 4.7 4.7 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 9778 None 0 Human Binding pKi = 4.7 4.7 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 9778 None 0 Human Binding pKi = 4.7 4.7 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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
60838 183874 None 99 Human Binding pKi = 6.7 6.7 1 2
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
CHEMBL481 183874 None 99 Human Binding pKi = 6.7 6.7 1 2
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC nan
135398745 2914 None 112 Human Binding pKi = 7.7 7.7 -32 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
135398745.0 2914 None 112 Human Binding pKi = 7.7 7.7 -32 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2914 None 112 Human Binding pKi = 7.7 7.7 -32 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2914 None 112 Human Binding pKi = 7.7 7.7 -32 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2914 None 112 Human Binding pKi = 7.7 7.7 -32 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
145961161 161606 None 0 Human Binding pKi = 7.6 7.6 -2 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161606 None 0 Human Binding pKi = 7.6 7.6 -2 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
4735 195115 None 96 Human Binding pKi = 6.7 6.7 -6 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL361506 195115 None 96 Human Binding pKi = 6.7 6.7 -6 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL55 195115 None 96 Human Binding pKi = 6.7 6.7 -6 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
15050941 203667 None 0 Rat Binding pKi = 6.7 6.7 1 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 427 4 1 5 3.1 O=C1Nc2cccnc2N(C(=O)CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL67381 203667 None 0 Rat Binding pKi = 6.7 6.7 1 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 427 4 1 5 3.1 O=C1Nc2cccnc2N(C(=O)CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm00111a032
2337 3256 None 77 Human Binding pKi = 6.7 6.7 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3256 None 77 Human Binding pKi = 6.7 6.7 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3256 None 77 Human Binding pKi = 6.7 6.7 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002.0 3256 None 77 Human Binding pKi = 6.7 6.7 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3256 None 77 Human Binding pKi = 6.7 6.7 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3256 None 77 Human Binding pKi = 6.7 6.7 -26 62
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
44318766 205751 None 0 Human Binding pKi = 5.7 5.7 3 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
CHEMBL82754 205751 None 0 Human Binding pKi = 5.7 5.7 3 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
10262466 98344 None 0 Human Binding pKi = 6.7 6.7 -3 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 208 2 0 3 0.3 O=C1CCON1CC#CCN1CCCC1 10.1016/j.bmc.2007.09.003
CHEMBL275104 98344 None 0 Human Binding pKi = 6.7 6.7 -3 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 208 2 0 3 0.3 O=C1CCON1CC#CCN1CCCC1 10.1016/j.bmc.2007.09.003
44274468 80606 None 0 Human Binding pKi = 4.7 4.7 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 80606 None 0 Human Binding pKi = 4.7 4.7 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
44448498 12339 None 0 Human Binding pKi = 4.7 4.7 1 3
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12339 None 0 Human Binding pKi = 4.7 4.7 1 3
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12339 None 0 Human Binding pKi = 4.7 4.7 1 3
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
2750 204061 None 76 Human Binding pKi = 5.6 5.6 -1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 204061 None 76 Human Binding pKi = 5.6 5.6 -1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
44437308 12327 None 0 Human Binding pKi = 5.6 5.6 -4 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 12327 None 0 Human Binding pKi = 5.6 5.6 -4 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 12327 None 0 Human Binding pKi = 5.6 5.6 -4 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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
44448496 11912 None 0 Human Binding pKi = 4.6 4.6 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11912 None 0 Human Binding pKi = 4.6 4.6 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11912 None 0 Human Binding pKi = 4.6 4.6 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
9308 17754 None 21 Human Binding pKi = 7.6 7.6 -10 7
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
CHEMBL1255785 17754 None 21 Human Binding pKi = 7.6 7.6 -10 7
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
CHEMBL12587 17754 None 21 Human Binding pKi = 7.6 7.6 -10 7
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
CHEMBL292911 17754 None 21 Human Binding pKi = 7.6 7.6 -10 7
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9904001
15050953 102339 None 0 Rat Binding pKi = 7.6 7.6 -1 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 536 9 2 7 4.0 CC(C)(C)OC(=O)NCCCCCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL303684 102339 None 0 Rat Binding pKi = 7.6 7.6 -1 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 536 9 2 7 4.0 CC(C)(C)OC(=O)NCCCCCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
155516383 176673 None 0 Human Binding pKi = 7.6 7.6 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176673 None 0 Human Binding pKi = 7.6 7.6 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176673 None 0 Human Binding pKi = 7.6 7.6 -5 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
1548953 207679 None 27 Human Binding pKi = 6.6 6.6 -1 17
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 207679 None 27 Human Binding pKi = 6.6 6.6 -1 17
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
44318929 106862 None 0 Human Binding pKi = 5.6 5.6 2 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
CHEMBL314493 106862 None 0 Human Binding pKi = 5.6 5.6 2 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
71463061 83795 None 0 Human Binding pKi = 5.6 5.6 -3 9
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205813 83795 None 0 Human Binding pKi = 5.6 5.6 -3 9
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
44627958 14036 None 0 Human Binding pKi = 5.6 5.6 -7 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14036 None 0 Human Binding pKi = 5.6 5.6 -7 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14036 None 0 Human Binding pKi = 5.6 5.6 -7 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
10880435 59059 None 0 Human Binding pKi = 5.6 5.6 -10 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 59059 None 0 Human Binding pKi = 5.6 5.6 -10 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
2551 794 None 23 Human Binding pKi = 7.6 7.6 -21 11
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
2551.0 794 None 23 Human Binding pKi = 7.6 7.6 -21 11
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
298 794 None 23 Human Binding pKi = 7.6 7.6 -21 11
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
488 794 None 23 Human Binding pKi = 7.6 7.6 -21 11
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
CHEMBL965 794 None 23 Human Binding pKi = 7.6 7.6 -21 11
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
DB00411 794 None 23 Human Binding pKi = 7.6 7.6 -21 11
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
16086005 139231 None 0 Human Binding pKi = 7.6 7.6 -19 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 139231 None 0 Human Binding pKi = 7.6 7.6 -19 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
164616974 188518 None 0 Human Binding pKi = 7.6 7.6 -9 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 675 15 7 8 2.2 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4857722 188518 None 0 Human Binding pKi = 7.6 7.6 -9 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 675 15 7 8 2.2 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028407 188518 None 0 Human Binding pKi = 7.6 7.6 -9 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 675 15 7 8 2.2 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
2230 465 None 60 Human Binding pKi = 5.6 5.6 -218 10
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
296 465 None 60 Human Binding pKi = 5.6 5.6 -218 10
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
CHEMBL7303 465 None 60 Human Binding pKi = 5.6 5.6 -218 10
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
DB04365 465 None 60 Human Binding pKi = 5.6 5.6 -218 10
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
2230 465 None 60 Rat Binding pKi = 5.6 5.6 -562 10
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
296 465 None 60 Rat Binding pKi = 5.6 5.6 -562 10
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
CHEMBL7303 465 None 60 Rat Binding pKi = 5.6 5.6 -562 10
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
DB04365 465 None 60 Rat Binding pKi = 5.6 5.6 -562 10
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
2230 465 None 60 Human Binding pKi = 5.6 5.6 -218 10
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
296 465 None 60 Human Binding pKi = 5.6 5.6 -218 10
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
CHEMBL7303 465 None 60 Human Binding pKi = 5.6 5.6 -218 10
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
DB04365 465 None 60 Human Binding pKi = 5.6 5.6 -218 10
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
44326733 111629 None 0 Human Binding pKi = 4.6 4.6 -2691 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 306 2 2 3 3.3 c1ccc2c3c([nH]c2c1)C(Cc1ccc2c(c1)OCO2)NCC3 10.1016/j.bmcl.2007.01.093
CHEMBL328476 111629 None 0 Human Binding pKi = 4.6 4.6 -2691 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 306 2 2 3 3.3 c1ccc2c3c([nH]c2c1)C(Cc1ccc2c(c1)OCO2)NCC3 10.1016/j.bmcl.2007.01.093
191 403 None 98 Human Binding pKi = 6.6 6.6 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 403 None 98 Human Binding pKi = 6.6 6.6 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 403 None 98 Human Binding pKi = 6.6 6.6 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170.0 403 None 98 Human Binding pKi = 6.6 6.6 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 403 None 98 Human Binding pKi = 6.6 6.6 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 403 None 98 Human Binding pKi = 6.6 6.6 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
44578707 182141 None 0 Human Binding pKi = 5.6 5.6 -3 3
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 405 2 1 5 2.9 CN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)[C@@H]2CCCC[C@@H]21 10.1016/j.bmc.2008.06.025
CHEMBL478227 182141 None 0 Human Binding pKi = 5.6 5.6 -3 3
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 405 2 1 5 2.9 CN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)[C@@H]2CCCC[C@@H]21 10.1016/j.bmc.2008.06.025
9817231 158236 None 22 Human Binding pKi = 4.6 4.6 -2 7
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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 158236 None 22 Human Binding pKi = 4.6 4.6 -2 7
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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
44274433 99510 None 0 Human Binding pKi = 4.6 4.6 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 99510 None 0 Human Binding pKi = 4.6 4.6 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
24894632 189419 None 2 Human Binding pKi = 4.6 4.6 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc(C2CCCN2C)o1 10.1021/jm800145d
CHEMBL513277 189419 None 2 Human Binding pKi = 4.6 4.6 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc(C2CCCN2C)o1 10.1021/jm800145d
155562285 175842 None 0 Human Binding pKi = 7.6 7.6 -3 5
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M4 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 175842 None 0 Human Binding pKi = 7.6 7.6 -3 5
Displacement of [3H]NMS from human M4 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M4 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
44418764 82159 None 0 Human Binding pKi = 7.6 7.6 1 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 82159 None 0 Human Binding pKi = 7.6 7.6 1 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
25025581 201996 None 0 Human Binding pKi = 6.6 6.6 -3 8
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 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 201996 None 0 Human Binding pKi = 6.6 6.6 -3 8
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
164617938 188526 None 0 Human Binding pKi = 5.6 5.6 -17 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4854179 188526 None 0 Human Binding pKi = 5.6 5.6 -17 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028470 188526 None 0 Human Binding pKi = 5.6 5.6 -17 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156015968 178245 None 0 Human Binding pKi = 5.6 5.6 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178245 None 0 Human Binding pKi = 5.6 5.6 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178245 None 0 Human Binding pKi = 5.6 5.6 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
6604789 101047 None 5 Human Binding pKi = 4.6 4.6 -100 10
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 101047 None 5 Human Binding pKi = 4.6 4.6 -100 10
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
57326140 77179 None 0 Human Binding pKi = 4.6 4.6 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77179 None 0 Human Binding pKi = 4.6 4.6 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77179 None 0 Human Binding pKi = 4.6 4.6 -3 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
155528270 176391 None 0 Human Binding pKi = 6.6 6.6 -21 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176391 None 0 Human Binding pKi = 6.6 6.6 -21 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176391 None 0 Human Binding pKi = 6.6 6.6 -21 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
47358375 180762 None 1 Human Binding pKi = 6.6 6.6 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180762 None 1 Human Binding pKi = 6.6 6.6 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
44593620 187936 None 0 Human Binding pKi = 6.6 6.6 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187936 None 0 Human Binding pKi = 6.6 6.6 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
145961981 161531 None 0 Human Binding pKi = 6.6 6.6 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161531 None 0 Human Binding pKi = 6.6 6.6 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
15050950 204057 None 0 Rat Binding pKi = 5.6 5.6 -3 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 422 5 2 6 1.1 CC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL70003 204057 None 0 Rat Binding pKi = 5.6 5.6 -3 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 422 5 2 6 1.1 CC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
164614732 188498 None 0 Human Binding pKi = 4.6 4.6 -10 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 519 7 3 7 1.1 NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4860752 188498 None 0 Human Binding pKi = 4.6 4.6 -10 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 519 7 3 7 1.1 NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028266 188498 None 0 Human Binding pKi = 4.6 4.6 -10 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 519 7 3 7 1.1 NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
162658112 181071 None 0 Human Binding pKi = 4.6 4.6 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181071 None 0 Human Binding pKi = 4.6 4.6 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
46227483 14125 None 0 Human Binding pKi = 4.6 4.6 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14125 None 0 Human Binding pKi = 4.6 4.6 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14125 None 0 Human Binding pKi = 4.6 4.6 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
49783415 17678 None 0 Human Binding pKi = 5.6 5.6 -1071 12
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 17678 None 0 Human Binding pKi = 5.6 5.6 -1071 12
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
2247 505 None 81 Human Binding pKi = 6.6 6.6 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 None 81 Human Binding pKi = 6.6 6.6 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 None 81 Human Binding pKi = 6.6 6.6 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 None 81 Human Binding pKi = 6.6 6.6 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 None 81 Human Binding pKi = 6.6 6.6 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2230 465 None 60 Human Binding pKi = 7.6 7.6 -218 10
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
296 465 None 60 Human Binding pKi = 7.6 7.6 -218 10
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
CHEMBL7303 465 None 60 Human Binding pKi = 7.6 7.6 -218 10
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
DB04365 465 None 60 Human Binding pKi = 7.6 7.6 -218 10
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9904001
154734599 2503 None 12 Rat Binding pKi = 7.6 7.6 -3 11
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
327 2503 None 12 Rat Binding pKi = 7.6 7.6 -3 11
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
4108 2503 None 12 Rat Binding pKi = 7.6 7.6 -3 11
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
CHEMBL27673 2503 None 12 Rat Binding pKi = 7.6 7.6 -3 11
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
118719920 115773 None 0 Human Binding pKi = 7.6 7.6 2 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115773 None 0 Human Binding pKi = 7.6 7.6 2 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
154734599 2503 None 12 Rat Binding pKi = 7.6 7.6 -3 11
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
327 2503 None 12 Rat Binding pKi = 7.6 7.6 -3 11
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
4108 2503 None 12 Rat Binding pKi = 7.6 7.6 -3 11
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
CHEMBL27673 2503 None 12 Rat Binding pKi = 7.6 7.6 -3 11
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
CHEMBL306462 102965 None 0 Human Binding pKi = 5.6 5.6 -2 5
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 211 2 1 4 1.1 CCO/C(O)=C1\CN2CCCC(C2)C1=O 10.1021/jm020572p
2551 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
2551.0 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
298 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
488 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
CHEMBL965 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
DB00411 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9904001
2551 794 None 23 Rat Binding pKi = 5.6 5.6 -32 11
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
2551.0 794 None 23 Rat Binding pKi = 5.6 5.6 -32 11
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
298 794 None 23 Rat Binding pKi = 5.6 5.6 -32 11
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
488 794 None 23 Rat Binding pKi = 5.6 5.6 -32 11
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
CHEMBL965 794 None 23 Rat Binding pKi = 5.6 5.6 -32 11
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
DB00411 794 None 23 Rat Binding pKi = 5.6 5.6 -32 11
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
2551 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
2551.0 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
298 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
488 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
CHEMBL965 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
DB00411 794 None 23 Human Binding pKi = 5.6 5.6 -21 11
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
137644962 158493 None 0 Human Binding pKi = 5.6 5.6 -131 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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 158493 None 0 Human Binding pKi = 5.6 5.6 -131 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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
132060776 162402 None 0 Human Binding pKi = 5.6 5.6 -9 16
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 162402 None 0 Human Binding pKi = 5.6 5.6 -9 16
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
44448380 11915 None 0 Human Binding pKi = 5.6 5.6 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11915 None 0 Human Binding pKi = 5.6 5.6 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11915 None 0 Human Binding pKi = 5.6 5.6 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
122387444 138197 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 353 6 2 5 3.9 CCCCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
CHEMBL3769740 138197 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 353 6 2 5 3.9 CCCCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
10870954 120310 None 0 Human Binding pKi = 4.6 4.6 -1 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120310 None 0 Human Binding pKi = 4.6 4.6 -1 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
155560013 176300 None 0 Human Binding pKi = 7.6 7.6 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176300 None 0 Human Binding pKi = 7.6 7.6 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176300 None 0 Human Binding pKi = 7.6 7.6 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
CHEMBL69452 203974 None 0 Human Binding pKi = 6.6 6.6 -2 5
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 331 6 1 5 2.7 CCO/C(O)=C1\CN2CC(CCC2COCc2ccccc2)C1=O 10.1021/jm020572p
122387444 138197 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 353 6 2 5 3.9 CCCCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
CHEMBL3769740 138197 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 353 6 2 5 3.9 CCCCOc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1039/C5MD00334B
145961126 161553 None 0 Human Binding pKi = 5.6 5.6 -4 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161553 None 0 Human Binding pKi = 5.6 5.6 -4 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
1210 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
1213 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2725 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036.0 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
4411 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
616 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
6976 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
716121 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 918 None 51 Human Binding pKi = 6.6 6.6 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
237 204865 None 48 Human Binding pKi = 6.6 6.6 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 204865 None 48 Human Binding pKi = 6.6 6.6 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 204865 None 48 Human Binding pKi = 6.6 6.6 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 204865 None 48 Human Binding pKi = 6.6 6.6 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
73347827 92544 None 0 Human Binding pKi = 5.6 5.6 -1 4
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 311 4 0 2 2.6 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432052 92544 None 0 Human Binding pKi = 5.6 5.6 -1 4
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 311 4 0 2 2.6 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
44439402 169378 None 0 Human Binding pKi = 5.6 5.6 -1 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 292 2 1 2 3.4 OC1CCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL442093 169378 None 0 Human Binding pKi = 5.6 5.6 -1 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 292 2 1 2 3.4 OC1CCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
9308 17754 None 21 Human Binding pKi = 4.6 4.6 -10 7
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 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 17754 None 21 Human Binding pKi = 4.6 4.6 -10 7
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 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 17754 None 21 Human Binding pKi = 4.6 4.6 -10 7
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 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 17754 None 21 Human Binding pKi = 4.6 4.6 -10 7
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 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
44593622 187796 None 0 Human Binding pKi = 6.6 6.6 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187796 None 0 Human Binding pKi = 6.6 6.6 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187796 None 0 Human Binding pKi = 6.6 6.6 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
24894635 169807 None 0 Human Binding pKi = 4.6 4.6 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 169807 None 0 Human Binding pKi = 4.6 4.6 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 169807 None 0 Human Binding pKi = 4.6 4.6 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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
611101 203879 None 3 Rat Binding pKi = 5.6 5.6 -2 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 380 4 2 6 0.9 NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL68771 203879 None 3 Rat Binding pKi = 5.6 5.6 -2 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 380 4 2 6 0.9 NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
73353378 89802 None 0 Human Binding pKi = 6.5 6.5 -25 3
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 89802 None 0 Human Binding pKi = 6.5 6.5 -25 3
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
71463022 83698 None 7 Human Binding pKi = 5.5 5.5 -3 4
Displacement of [3H]QNB from human recombinant M4 receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]QNB from human recombinant M4 receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 436 8 0 5 5.3 COc1cc2oc(C(=O)N(CCCN3CCCCC3)c3ccccc3)c(C)c2cc1OC 10.1016/j.bmc.2012.09.044
CHEMBL2205362 83698 None 7 Human Binding pKi = 5.5 5.5 -3 4
Displacement of [3H]QNB from human recombinant M4 receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]QNB from human recombinant M4 receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 436 8 0 5 5.3 COc1cc2oc(C(=O)N(CCCN3CCCCC3)c3ccccc3)c(C)c2cc1OC 10.1016/j.bmc.2012.09.044
135 2532 None 43 Human Binding pKi = 6.5 6.5 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2532 None 43 Human Binding pKi = 6.5 6.5 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2532 None 43 Human Binding pKi = 6.5 6.5 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184.0 2532 None 43 Human Binding pKi = 6.5 6.5 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2532 None 43 Human Binding pKi = 6.5 6.5 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2532 None 43 Human Binding pKi = 6.5 6.5 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
109014373 179802 None 1 Human Binding pKi = 6.5 6.5 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 179802 None 1 Human Binding pKi = 6.5 6.5 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
44448646 11908 None 0 Human Binding pKi = 6.5 6.5 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11908 None 0 Human Binding pKi = 6.5 6.5 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11908 None 0 Human Binding pKi = 6.5 6.5 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
16085999 80292 None 0 Human Binding pKi = 7.5 7.5 -60 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 80292 None 0 Human Binding pKi = 7.5 7.5 -60 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
155513986 176487 None 0 Human Binding pKi = 7.5 7.5 -17 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176487 None 0 Human Binding pKi = 7.5 7.5 -17 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176487 None 0 Human Binding pKi = 7.5 7.5 -17 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
135409468 2035 None 69 Human Binding pKi = 6.5 6.5 -79 39
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 2035 None 69 Human Binding pKi = 6.5 6.5 -79 39
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 2035 None 69 Human Binding pKi = 6.5 6.5 -79 39
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
16086004 139237 None 0 Human Binding pKi = 6.5 6.5 -77 3
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 139237 None 0 Human Binding pKi = 6.5 6.5 -77 3
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
11751922 73074 None 19 Human Binding pKi = 5.5 5.5 -5 2
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 477 4 2 7 4.7 CC(C)Cn1c2ccc(Nc3ncccn3)cc2c2c3c(c4c(c21)CCc1nn(C)cc1-4)C(=O)NC3 10.1021/jm201449n
CHEMBL2010872 73074 None 19 Human Binding pKi = 5.5 5.5 -5 2
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 477 4 2 7 4.7 CC(C)Cn1c2ccc(Nc3ncccn3)cc2c2c3c(c4c(c21)CCc1nn(C)cc1-4)C(=O)NC3 10.1021/jm201449n
15050946 102646 None 0 Rat Binding pKi = 5.5 5.5 -1 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 484 5 2 6 2.5 CNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
CHEMBL304391 102646 None 0 Rat Binding pKi = 5.5 5.5 -1 4
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 484 5 2 6 2.5 CNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
10104 3566 None 12 Human Binding pKi = 6.5 6.5 -9 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 3566 None 12 Human Binding pKi = 6.5 6.5 -9 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 3566 None 12 Human Binding pKi = 6.5 6.5 -9 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
155552923 176307 None 0 Human Binding pKi = 6.5 6.5 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176307 None 0 Human Binding pKi = 6.5 6.5 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176307 None 0 Human Binding pKi = 6.5 6.5 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
164627658 188609 None 0 Human Binding pKi = 5.5 5.5 -72 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4875268 188609 None 0 Human Binding pKi = 5.5 5.5 -72 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5029013 188609 None 0 Human Binding pKi = 5.5 5.5 -72 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 22 9 12 0.6 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164628906 188616 None 0 Human Binding pKi = 5.5 5.5 -56 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 20 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(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4877107 188616 None 0 Human Binding pKi = 5.5 5.5 -56 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 20 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(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5029079 188616 None 0 Human Binding pKi = 5.5 5.5 -56 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 20 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(C(=O)CCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
57326146 77187 None 0 Human Binding pKi = 4.5 4.5 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77187 None 0 Human Binding pKi = 4.5 4.5 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77187 None 0 Human Binding pKi = 4.5 4.5 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
7141656 176837 None 7 Human Binding pKi = 4.5 4.5 -9 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 176837 None 7 Human Binding pKi = 4.5 4.5 -9 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc([C@H]2CCCN2)o1 10.1021/jm800145d
3198 205513 None 76 Human Binding pKi = 6.5 6.5 -8 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205513 None 76 Human Binding pKi = 6.5 6.5 -8 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205513 None 76 Human Binding pKi = 6.5 6.5 -8 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
71452384 83797 None 0 Human Binding pKi = 5.5 5.5 -14 5
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
CHEMBL2205816 83797 None 0 Human Binding pKi = 5.5 5.5 -14 5
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
71452384 83797 None 0 Human Binding pKi = 5.5 5.5 -14 5
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
CHEMBL2205816 83797 None 0 Human Binding pKi = 5.5 5.5 -14 5
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
174174 523 None 49 Human Binding pKi = 8.5 8.5 -2 14
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 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
174174.0 523 None 49 Human Binding pKi = 8.5 8.5 -2 14
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 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
260 523 None 49 Human Binding pKi = 8.5 8.5 -2 14
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 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
320 523 None 49 Human Binding pKi = 8.5 8.5 -2 14
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 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 523 None 49 Human Binding pKi = 8.5 8.5 -2 14
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 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 523 None 49 Human Binding pKi = 8.5 8.5 -2 14
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 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
10949838 5221 None 0 Human Binding pKi = 8.5 8.5 72 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5221 None 0 Human Binding pKi = 8.5 8.5 72 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
10225881 107621 None 0 Human Binding pKi = 8.5 8.5 112 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 450 6 1 5 5.9 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL318995 107621 None 0 Human Binding pKi = 8.5 8.5 112 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 450 6 1 5 5.9 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
164627445 188607 None 0 Human Binding pKi = 8.5 8.5 -14 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188607 None 0 Human Binding pKi = 8.5 8.5 -14 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188607 None 0 Human Binding pKi = 8.5 8.5 -14 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
2705 3842 None 64 Human Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 3842 None 64 Human Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 3842 None 64 Human Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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
443879.0 3842 None 64 Human Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 3842 None 64 Human Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 3842 None 64 Human Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 3842 None 64 Rat Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 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 3842 None 64 Rat Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 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 3842 None 64 Rat Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 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
443879.0 3842 None 64 Rat Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 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 3842 None 64 Rat Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 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 3842 None 64 Rat Binding pKi = 8.5 8.5 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 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
164626501 188596 None 0 Human Binding pKi = 8.5 8.5 -17 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCNC(=N)N)N[C@@H](CCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4874955 188596 None 0 Human Binding pKi = 8.5 8.5 -17 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCNC(=N)N)N[C@@H](CCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028936 188596 None 0 Human Binding pKi = 8.5 8.5 -17 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCNC(=N)N)N[C@@H](CCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
155539713 176360 None 0 Human Binding pKi = 8.5 8.5 -28 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176360 None 0 Human Binding pKi = 8.5 8.5 -28 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176360 None 0 Human Binding pKi = 8.5 8.5 -28 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
CHEMBL5283759 194228 None 0 Human Binding pKi = 8.5 8.5 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1024 19 1 13 9.4 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCN6CCC(OC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
16115950 136382 None 0 Human Binding pKi = 8.5 8.5 1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 136382 None 0 Human Binding pKi = 8.5 8.5 1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
164611865 188476 None 0 Human Binding pKi = 8.5 8.5 -41 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4856113 188476 None 0 Human Binding pKi = 8.5 8.5 -41 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028107 188476 None 0 Human Binding pKi = 8.5 8.5 -41 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
16115801 12295 None 0 Human Binding pKi = 8.5 8.5 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 12295 None 0 Human Binding pKi = 8.5 8.5 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 12295 None 0 Human Binding pKi = 8.5 8.5 -1 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
164618444 188529 None 0 Human Binding pKi = 8.5 8.5 -16 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 873 21 9 11 1.9 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4852186 188529 None 0 Human Binding pKi = 8.5 8.5 -16 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 873 21 9 11 1.9 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028499 188529 None 0 Human Binding pKi = 8.5 8.5 -16 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 873 21 9 11 1.9 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
2774 3868 None 95 Human Binding pKi = 8.5 8.5 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
5593 3868 None 95 Human Binding pKi = 8.5 8.5 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
5593.0 3868 None 95 Human Binding pKi = 8.5 8.5 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
7319 3868 None 95 Human Binding pKi = 8.5 8.5 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
CHEMBL1200604 3868 None 95 Human Binding pKi = 8.5 8.5 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB00809 3868 None 95 Human Binding pKi = 8.5 8.5 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB01199 3868 None 95 Human Binding pKi = 8.5 8.5 1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
155543944 176334 None 0 Human Binding pKi = 8.5 8.5 -10 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176334 None 0 Human Binding pKi = 8.5 8.5 -10 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176334 None 0 Human Binding pKi = 8.5 8.5 -10 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
2028 2979 None 80 Human Binding pKi = 8.4 8.4 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 2979 None 80 Human Binding pKi = 8.4 8.4 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 2979 None 80 Human Binding pKi = 8.4 8.4 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
4634.0 2979 None 80 Human Binding pKi = 8.4 8.4 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 2979 None 80 Human Binding pKi = 8.4 8.4 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 2979 None 80 Human Binding pKi = 8.4 8.4 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
137628879 160972 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 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 160972 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 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 160972 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 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 160972 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M4 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M4 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
5648 78411 None 9 Human Binding pKi = 8.4 8.4 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 78411 None 9 Human Binding pKi = 8.4 8.4 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 78411 None 9 Human Binding pKi = 8.4 8.4 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
162677513 183744 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183744 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183744 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
CHEMBL5267836 193538 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1038 20 1 13 9.8 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(OC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
164616463 188514 None 0 Human Binding pKi = 8.4 8.4 -36 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 860 22 9 12 0.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)NC(=O)[C@@H](N)CCCN 10.1016/j.ejmech.2021.113159
CHEMBL4859378 188514 None 0 Human Binding pKi = 8.4 8.4 -36 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 860 22 9 12 0.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)NC(=O)[C@@H](N)CCCN 10.1016/j.ejmech.2021.113159
CHEMBL5028381 188514 None 0 Human Binding pKi = 8.4 8.4 -36 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 860 22 9 12 0.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)NC(=O)[C@@H](N)CCCN 10.1016/j.ejmech.2021.113159
164628529 188614 None 0 Human Binding pKi = 8.4 8.4 -18 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 914 17 9 12 0.2 CC(=O)NC(=O)[C@H](CCNC(=N)N)NC(=O)[C@@H]1CC(=O)NCCC[C@@H](C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)N1 10.1016/j.ejmech.2021.113159
CHEMBL4876725 188614 None 0 Human Binding pKi = 8.4 8.4 -18 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 914 17 9 12 0.2 CC(=O)NC(=O)[C@H](CCNC(=N)N)NC(=O)[C@@H]1CC(=O)NCCC[C@@H](C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)N1 10.1016/j.ejmech.2021.113159
CHEMBL5029058 188614 None 0 Human Binding pKi = 8.4 8.4 -18 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 914 17 9 12 0.2 CC(=O)NC(=O)[C@H](CCNC(=N)N)NC(=O)[C@@H]1CC(=O)NCCC[C@@H](C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)N1 10.1016/j.ejmech.2021.113159
164616706 188515 None 0 Human Binding pKi = 8.4 8.4 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188515 None 0 Human Binding pKi = 8.4 8.4 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188515 None 0 Human Binding pKi = 8.4 8.4 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
156015153 178307 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178307 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178307 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
44627853 197681 None 0 Human Binding pKi = 8.4 8.4 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 197681 None 0 Human Binding pKi = 8.4 8.4 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
10862395 5026 None 0 Human Binding pKi = 8.4 8.4 22 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5026 None 0 Human Binding pKi = 8.4 8.4 22 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 406 4 1 5 4.4 CCOC(=O)c1c(CC)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
11767229 78917 None 0 Human Binding pKi = 7.5 7.5 -30 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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 78917 None 0 Human Binding pKi = 7.5 7.5 -30 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 607 15 2 3 7.5 O=C(CCCCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
156015390 178242 None 0 Human Binding pKi = 7.5 7.5 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178242 None 0 Human Binding pKi = 7.5 7.5 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178242 None 0 Human Binding pKi = 7.5 7.5 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
44439408 91215 None 0 Human Binding pKi = 6.5 6.5 -1 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 426 4 0 5 4.9 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C1SCCSC1C3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL240024 91215 None 0 Human Binding pKi = 6.5 6.5 -1 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 426 4 0 5 4.9 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C1SCCSC1C3)CC2 10.1016/j.bmcl.2007.01.093
9950396 145123 None 0 Human Binding pKi = 6.5 6.5 1 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 352 4 1 4 3.4 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(O)CC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL391192 145123 None 0 Human Binding pKi = 6.5 6.5 1 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 352 4 1 4 3.4 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(O)CC3)CC2 10.1016/j.bmcl.2007.01.093
11773414 147285 None 0 Human Binding pKi = 6.5 6.5 2 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 380 4 1 4 4.2 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(O)CCCC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL392887 147285 None 0 Human Binding pKi = 6.5 6.5 2 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 380 4 1 4 4.2 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(O)CCCC3)CC2 10.1016/j.bmcl.2007.01.093
44318930 106172 None 0 Human Binding pKi = 6.5 6.5 2 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
CHEMBL313738 106172 None 0 Human Binding pKi = 6.5 6.5 2 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
11184481 201428 None 15 Human Binding pKi = 5.5 5.5 1 4
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 258 1 0 5 1.8 Cc1ccc2oc(N3CCN4CCC3CC4)nc2n1 10.1021/jm9015075
CHEMBL604798 201428 None 15 Human Binding pKi = 5.5 5.5 1 4
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 258 1 0 5 1.8 Cc1ccc2oc(N3CCN4CCC3CC4)nc2n1 10.1021/jm9015075
156013387 178261 None 0 Human Binding pKi = 5.5 5.5 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178261 None 0 Human Binding pKi = 5.5 5.5 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178261 None 0 Human Binding pKi = 5.5 5.5 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
46227485 14123 None 0 Human Binding pKi = 4.5 4.5 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14123 None 0 Human Binding pKi = 4.5 4.5 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14123 None 0 Human Binding pKi = 4.5 4.5 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
44593626 187853 None 0 Human Binding pKi = 6.5 6.5 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187853 None 0 Human Binding pKi = 6.5 6.5 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187853 None 0 Human Binding pKi = 6.5 6.5 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
CHEMBL4520788 213975 None 10 Human Binding pKi = 6.5 6.5 -14 25
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a CHRM4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a CHRM4
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
164622170 188560 None 0 Human Binding pKi = 6.5 6.5 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 846 20 9 12 -0.4 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4863723 188560 None 0 Human Binding pKi = 6.5 6.5 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 846 20 9 12 -0.4 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028687 188560 None 0 Human Binding pKi = 6.5 6.5 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 846 20 9 12 -0.4 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44627856 197489 None 0 Human Binding pKi = 5.5 5.5 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 197489 None 0 Human Binding pKi = 5.5 5.5 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
46227413 14140 None 0 Human Binding pKi = 4.5 4.5 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14140 None 0 Human Binding pKi = 4.5 4.5 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14140 None 0 Human Binding pKi = 4.5 4.5 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
11828362 78920 None 0 Human Binding pKi = 7.5 7.5 -40 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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 78920 None 0 Human Binding pKi = 7.5 7.5 -40 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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
16086062 80791 None 0 Human Binding pKi = 7.5 7.5 -58 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 80791 None 0 Human Binding pKi = 7.5 7.5 -58 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
9909908 13519 None 0 Human Binding pKi = 7.5 7.5 -1 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
CHEMBL1193635 13519 None 0 Human Binding pKi = 7.5 7.5 -1 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
CHEMBL545077 13519 None 0 Human Binding pKi = 7.5 7.5 -1 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
10373706 57409 None 0 Rat Binding pKi = 7.5 7.5 -6 4
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell 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 57409 None 0 Rat Binding pKi = 7.5 7.5 -6 4
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell 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
44593624 188129 None 0 Human Binding pKi = 6.5 6.5 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 188129 None 0 Human Binding pKi = 6.5 6.5 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 188129 None 0 Human Binding pKi = 6.5 6.5 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
44593616 193214 None 0 Human Binding pKi = 6.5 6.5 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 193214 None 0 Human Binding pKi = 6.5 6.5 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
122387449 138249 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 327 5 2 5 3.4 CCCCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
CHEMBL3770360 138249 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 327 5 2 5 3.4 CCCCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
137636308 156202 None 0 Human Binding pKi = 5.5 5.5 -10 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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 156202 None 0 Human Binding pKi = 5.5 5.5 -10 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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
2736067 87530 None 73 Human Binding pKi = 4.5 4.5 -371 5
Displacement of [3H]-NMS from recombinant muscarinic M4 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-NMS from recombinant muscarinic M4 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 87530 None 73 Human Binding pKi = 4.5 4.5 -371 5
Displacement of [3H]-NMS from recombinant muscarinic M4 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-NMS from recombinant muscarinic M4 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
2381 663 None 48 Human Binding pKi = 7.5 7.5 -9 8
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
2381.0 663 None 48 Human Binding pKi = 7.5 7.5 -9 8
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
374 663 None 48 Human Binding pKi = 7.5 7.5 -9 8
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 663 None 48 Human Binding pKi = 7.5 7.5 -9 8
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 663 None 48 Human Binding pKi = 7.5 7.5 -9 8
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 663 None 48 Human Binding pKi = 7.5 7.5 -9 8
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
118719931 115785 None 0 Human Binding pKi = 7.5 7.5 -1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115785 None 0 Human Binding pKi = 7.5 7.5 -1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
154734599 2503 None 12 Rat Binding pKi = 7.5 7.5 -3 11
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
327 2503 None 12 Rat Binding pKi = 7.5 7.5 -3 11
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
4108 2503 None 12 Rat Binding pKi = 7.5 7.5 -3 11
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
CHEMBL27673 2503 None 12 Rat Binding pKi = 7.5 7.5 -3 11
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
122387449 138249 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 327 5 2 5 3.4 CCCCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
CHEMBL3770360 138249 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 327 5 2 5 3.4 CCCCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
11833737 120339 None 0 Human Binding pKi = 5.5 5.5 -1 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120339 None 0 Human Binding pKi = 5.5 5.5 -1 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
164615651 188511 None 0 Human Binding pKi = 5.5 5.5 -41 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4852079 188511 None 0 Human Binding pKi = 5.5 5.5 -41 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028329 188511 None 0 Human Binding pKi = 5.5 5.5 -41 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
9815331 203107 None 1 Human Binding pKi = 7.5 7.5 -4 8
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL64000 203107 None 1 Human Binding pKi = 7.5 7.5 -4 8
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
9815331 203107 None 1 Rat Binding pKi = 7.5 7.5 -12 8
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 203107 None 1 Rat Binding pKi = 7.5 7.5 -12 8
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
9815331 203107 None 1 Human Binding pKi = 7.5 7.5 -4 8
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 203107 None 1 Human Binding pKi = 7.5 7.5 -4 8
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
44627860 14035 None 0 Human Binding pKi = 7.5 7.5 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14035 None 0 Human Binding pKi = 7.5 7.5 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14035 None 0 Human Binding pKi = 7.5 7.5 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
44593619 187460 None 0 Human Binding pKi = 7.5 7.5 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187460 None 0 Human Binding pKi = 7.5 7.5 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
2200 3131 None 46 Rat Binding pKi = 6.5 6.5 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
328 3131 None 46 Rat Binding pKi = 6.5 6.5 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
4848 3131 None 46 Rat Binding pKi = 6.5 6.5 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
4848.0 3131 None 46 Rat Binding pKi = 6.5 6.5 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
CHEMBL9967 3131 None 46 Rat Binding pKi = 6.5 6.5 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
DB00670 3131 None 46 Rat Binding pKi = 6.5 6.5 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
11759212 57892 None 0 Human Binding pKi = 6.5 6.5 -407 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 57892 None 0 Human Binding pKi = 6.5 6.5 -407 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
44274317 83372 None 0 Human Binding pKi = 4.5 4.5 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 83372 None 0 Human Binding pKi = 4.5 4.5 -1 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
43815 186920 None 64 Human Binding pKi = 7.5 7.5 -8 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 186920 None 64 Human Binding pKi = 7.5 7.5 -8 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 186920 None 64 Human Binding pKi = 7.5 7.5 -8 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
2200 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
328 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
4848 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
4848.0 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
CHEMBL9967 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
DB00670 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
2200 3131 None 46 Human Binding pKi = 7.5 7.5 -2 12
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
328 3131 None 46 Human Binding pKi = 7.5 7.5 -2 12
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
4848 3131 None 46 Human Binding pKi = 7.5 7.5 -2 12
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
4848.0 3131 None 46 Human Binding pKi = 7.5 7.5 -2 12
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
CHEMBL9967 3131 None 46 Human Binding pKi = 7.5 7.5 -2 12
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
DB00670 3131 None 46 Human Binding pKi = 7.5 7.5 -2 12
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 CellCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
2200 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
328 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
4848 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
4848.0 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
CHEMBL9967 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
DB00670 3131 None 46 Rat Binding pKi = 7.5 7.5 -7 12
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
156021441 178154 None 0 Human Binding pKi = 7.5 7.5 -7 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178154 None 0 Human Binding pKi = 7.5 7.5 -7 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
424430 107629 None 5 Human Binding pKi = 4.5 4.5 -1318 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 292 3 2 2 3.6 COc1cccc(CC2NCCc3c2[nH]c2ccccc32)c1 10.1016/j.bmcl.2007.01.093
CHEMBL319005 107629 None 5 Human Binding pKi = 4.5 4.5 -1318 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 292 3 2 2 3.6 COc1cccc(CC2NCCc3c2[nH]c2ccccc32)c1 10.1016/j.bmcl.2007.01.093
9906447 195577 None 2 Human Binding pKi = 6.5 6.5 -478 13
Binding affinity to human recombinant M4 receptorBinding affinity to human recombinant M4 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031738 195577 None 2 Human Binding pKi = 6.5 6.5 -478 13
Binding affinity to human recombinant M4 receptorBinding affinity to human recombinant M4 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL555146 195577 None 2 Human Binding pKi = 6.5 6.5 -478 13
Binding affinity to human recombinant M4 receptorBinding affinity to human recombinant M4 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
73355415 92533 None 0 Human Binding pKi = 6.5 6.5 -1 13
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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 92533 None 0 Human Binding pKi = 6.5 6.5 -1 13
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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
164623942 188579 None 0 Human Binding pKi = 6.5 6.5 -26 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 11 10 0.9 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4873621 188579 None 0 Human Binding pKi = 6.5 6.5 -26 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 11 10 0.9 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028796 188579 None 0 Human Binding pKi = 6.5 6.5 -26 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 11 10 0.9 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
44593618 187459 None 0 Human Binding pKi = 6.5 6.5 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187459 None 0 Human Binding pKi = 6.5 6.5 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
73352415 92538 None 0 Human Binding pKi = 5.5 5.5 -1 4
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 293 4 0 2 2.5 CN(CCc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432044 92538 None 0 Human Binding pKi = 5.5 5.5 -1 4
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 293 4 0 2 2.5 CN(CCc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
2335 11848 None 22 Human Binding pKi = 7.4 7.4 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 11848 None 22 Human Binding pKi = 7.4 7.4 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 11848 None 22 Human Binding pKi = 7.4 7.4 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 11848 None 22 Human Binding pKi = 7.4 7.4 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10557581 21774 None 0 Rat Binding pKi = 7.4 7.4 -6 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL1202001 21774 None 0 Rat Binding pKi = 7.4 7.4 -6 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL131913 21774 None 0 Rat Binding pKi = 7.4 7.4 -6 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
11968014 12758 None 5 Human Binding pKi = 7.4 7.4 -12 9
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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
119680147.0 12758 None 5 Human Binding pKi = 7.4 7.4 -12 9
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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 12758 None 5 Human Binding pKi = 7.4 7.4 -12 9
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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
DB00747 12758 None 5 Human Binding pKi = 7.4 7.4 -12 9
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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
164619478 188539 None 0 Human Binding pKi = 6.4 6.4 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 533 8 3 7 1.5 NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4872882 188539 None 0 Human Binding pKi = 6.4 6.4 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 533 8 3 7 1.5 NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028552 188539 None 0 Human Binding pKi = 6.4 6.4 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 533 8 3 7 1.5 NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
11101362 5125 None 0 Human Binding pKi = 6.4 6.4 7 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5125 None 0 Human Binding pKi = 6.4 6.4 7 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Cl)ccc2C1O3 10.1021/jm011116o
68617 205527 None 62 Human Binding pKi = 6.4 6.4 -20 26
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 205527 None 62 Human Binding pKi = 6.4 6.4 -20 26
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 205527 None 62 Human Binding pKi = 6.4 6.4 -20 26
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
9872676 78195 None 0 Human Binding pKi = 5.4 5.4 -9332 16
Binding affinity to human M4 receptorBinding affinity to human M4 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 78195 None 0 Human Binding pKi = 5.4 5.4 -9332 16
Binding affinity to human M4 receptorBinding affinity to human M4 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
155557119 176511 None 0 Human Binding pKi = 7.4 7.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176511 None 0 Human Binding pKi = 7.4 7.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176511 None 0 Human Binding pKi = 7.4 7.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
11011757 59223 None 0 Human Binding pKi = 6.4 6.4 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 59223 None 0 Human Binding pKi = 6.4 6.4 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
44627956 14034 None 0 Human Binding pKi = 6.4 6.4 -7 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14034 None 0 Human Binding pKi = 6.4 6.4 -7 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14034 None 0 Human Binding pKi = 6.4 6.4 -7 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
156015465 178324 None 0 Human Binding pKi = 5.4 5.4 -1 4
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
CHEMBL4640926 178324 None 0 Human Binding pKi = 5.4 5.4 -1 4
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
CHEMBL4651115 178324 None 0 Human Binding pKi = 5.4 5.4 -1 4
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
154734599 2503 None 12 Human Binding pKi = 7.4 7.4 -2 11
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
327 2503 None 12 Human Binding pKi = 7.4 7.4 -2 11
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
4108 2503 None 12 Human Binding pKi = 7.4 7.4 -2 11
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
CHEMBL27673 2503 None 12 Human Binding pKi = 7.4 7.4 -2 11
Affinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M4 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
3055 1433 None 44 Human Binding pKi = 7.4 7.4 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
313 1433 None 44 Human Binding pKi = 7.4 7.4 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
7163 1433 None 44 Human Binding pKi = 7.4 7.4 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
CHEMBL936 1433 None 44 Human Binding pKi = 7.4 7.4 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
DB01231 1433 None 44 Human Binding pKi = 7.4 7.4 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
164611187 188470 None 0 Human Binding pKi = 7.4 7.4 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 17 8 9 1.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4851265 188470 None 0 Human Binding pKi = 7.4 7.4 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 17 8 9 1.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028060 188470 None 0 Human Binding pKi = 7.4 7.4 -2 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 17 8 9 1.3 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
44627748 14094 None 0 Human Binding pKi = 7.4 7.4 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14094 None 0 Human Binding pKi = 7.4 7.4 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14094 None 0 Human Binding pKi = 7.4 7.4 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
156015051 178328 None 0 Human Binding pKi = 5.4 5.4 -9 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178328 None 0 Human Binding pKi = 5.4 5.4 -9 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178328 None 0 Human Binding pKi = 5.4 5.4 -9 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178329 None 0 Human Binding pKi = 5.4 5.4 -9 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178329 None 0 Human Binding pKi = 5.4 5.4 -9 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178329 None 0 Human Binding pKi = 5.4 5.4 -9 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
73355419 92549 None 0 Human Binding pKi = 5.4 5.4 -4 5
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 4 0 2 2.7 CN(CCc1ccccn1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL2432059 92549 None 0 Human Binding pKi = 5.4 5.4 -4 5
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 4 0 2 2.7 CN(CCc1ccccn1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
11536903 2397 None 68 Human Binding pKi = 6.4 6.4 6 2
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
3262 2397 None 68 Human Binding pKi = 6.4 6.4 6 2
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
CHEMBL3770346 2397 None 68 Human Binding pKi = 6.4 6.4 6 2
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
118719927 115781 None 0 Human Binding pKi = 6.4 6.4 -3 8
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115781 None 0 Human Binding pKi = 6.4 6.4 -3 8
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
12963076 196625 None 4 Human Binding pKi = 5.4 5.4 -9332 7
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 196625 None 4 Human Binding pKi = 5.4 5.4 -9332 7
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
156011518 178338 None 0 Human Binding pKi = 5.4 5.4 -5 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178338 None 0 Human Binding pKi = 5.4 5.4 -5 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178338 None 0 Human Binding pKi = 5.4 5.4 -5 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
16086060 168943 None 0 Human Binding pKi = 7.4 7.4 -100 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 168943 None 0 Human Binding pKi = 7.4 7.4 -100 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
3652 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
57 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
60809 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
60809.0 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
CHEMBL21536 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
DB15357 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
155557119 176511 None 0 Human Binding pKi = 7.4 7.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 176511 None 0 Human Binding pKi = 7.4 7.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 176511 None 0 Human Binding pKi = 7.4 7.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
164620907 188548 None 0 Human Binding pKi = 7.4 7.4 -47 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188548 None 0 Human Binding pKi = 7.4 7.4 -47 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188548 None 0 Human Binding pKi = 7.4 7.4 -47 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
10486393 141702 None 0 Rat Binding pKi = 7.4 7.4 -43 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 141702 None 0 Rat Binding pKi = 7.4 7.4 -43 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 141702 None 0 Rat Binding pKi = 7.4 7.4 -43 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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
3652 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809.0 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4097 None 79 Human Binding pKi = 7.4 7.4 -3 18
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
10033774 56546 None 0 Rat Binding pKi = 7.4 7.4 1 4
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell 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 56546 None 0 Rat Binding pKi = 7.4 7.4 1 4
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell 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
73349362 92550 None 0 Human Binding pKi = 5.4 5.4 -1 2
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 311 5 0 1 3.8 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL2432060 92550 None 0 Human Binding pKi = 5.4 5.4 -1 2
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 311 5 0 1 3.8 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
2551 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
2551.0 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
298 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
488 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
CHEMBL965 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
DB00411 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
156012936 178296 None 0 Human Binding pKi = 6.4 6.4 -6 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178296 None 0 Human Binding pKi = 6.4 6.4 -6 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178296 None 0 Human Binding pKi = 6.4 6.4 -6 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
2551 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
2551.0 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 794 None 23 Human Binding pKi = 6.4 6.4 -21 11
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
10474335 194692 None 23 Human Binding pKi = 5.4 5.4 -138 10
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
CHEMBL53325 194692 None 23 Human Binding pKi = 5.4 5.4 -138 10
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
156015719 178258 None 0 Human Binding pKi = 5.4 5.4 -7 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178258 None 0 Human Binding pKi = 5.4 5.4 -7 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178258 None 0 Human Binding pKi = 5.4 5.4 -7 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
9815331 203107 None 1 Human Binding pKi = 8.4 8.4 -4 8
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL64000 203107 None 1 Human Binding pKi = 8.4 8.4 -4 8
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
164619001 188536 None 0 Human Binding pKi = 8.4 8.4 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 887 22 9 11 2.3 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4871153 188536 None 0 Human Binding pKi = 8.4 8.4 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 887 22 9 11 2.3 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028529 188536 None 0 Human Binding pKi = 8.4 8.4 -14 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 887 22 9 11 2.3 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164610955 188469 None 0 Human Binding pKi = 8.4 8.4 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 661 15 6 8 2.3 N=C(N)NCCC[C@@H](NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)O 10.1016/j.ejmech.2021.113159
CHEMBL4858398 188469 None 0 Human Binding pKi = 8.4 8.4 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 661 15 6 8 2.3 N=C(N)NCCC[C@@H](NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)O 10.1016/j.ejmech.2021.113159
CHEMBL5028048 188469 None 0 Human Binding pKi = 8.4 8.4 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 661 15 6 8 2.3 N=C(N)NCCC[C@@H](NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1)C(=O)O 10.1016/j.ejmech.2021.113159
44627858 14038 None 0 Human Binding pKi = 8.4 8.4 -6 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14038 None 0 Human Binding pKi = 8.4 8.4 -6 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14038 None 0 Human Binding pKi = 8.4 8.4 -6 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
162654942 183671 None 0 Human Binding pKi = 8.4 8.4 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183671 None 0 Human Binding pKi = 8.4 8.4 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 183671 None 0 Human Binding pKi = 8.4 8.4 -2 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
10316726 12028 None 0 Human Binding pKi = 8.4 8.4 -8 5
Compound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesCompound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
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 12028 None 0 Human Binding pKi = 8.4 8.4 -8 5
Compound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesCompound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
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 12028 None 0 Human Binding pKi = 8.4 8.4 -8 5
Compound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesCompound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
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
164617401 188520 None 0 Human Binding pKi = 8.4 8.4 -12 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 900 16 9 12 -0.2 CC(=O)NC(=O)[C@H](CCNC(=N)N)NC(=O)[C@@H]1CC(=O)NCCC[C@@H](C(=O)NCCN2CCN(CCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)N1 10.1016/j.ejmech.2021.113159
CHEMBL4852646 188520 None 0 Human Binding pKi = 8.4 8.4 -12 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 900 16 9 12 -0.2 CC(=O)NC(=O)[C@H](CCNC(=N)N)NC(=O)[C@@H]1CC(=O)NCCC[C@@H](C(=O)NCCN2CCN(CCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)N1 10.1016/j.ejmech.2021.113159
CHEMBL5028427 188520 None 0 Human Binding pKi = 8.4 8.4 -12 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 900 16 9 12 -0.2 CC(=O)NC(=O)[C@H](CCNC(=N)N)NC(=O)[C@@H]1CC(=O)NCCC[C@@H](C(=O)NCCN2CCN(CCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)N1 10.1016/j.ejmech.2021.113159
156016041 178247 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178247 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178247 None 0 Human Binding pKi = 8.4 8.4 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
15157138 99625 None 0 Human Binding pKi = 8.3 8.3 -1 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 345 9 0 3 4.8 CCN(CC)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL284137 99625 None 0 Human Binding pKi = 8.3 8.3 -1 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 345 9 0 3 4.8 CCN(CC)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
10316726 12028 None 0 Human Binding pKi = 8.3 8.3 -8 5
Compound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesCompound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
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 12028 None 0 Human Binding pKi = 8.3 8.3 -8 5
Compound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesCompound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
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 12028 None 0 Human Binding pKi = 8.3 8.3 -8 5
Compound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesCompound was tested for binding affinity against Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
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
56965018 77181 None 0 Human Binding pKi = 8.3 8.3 -2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77181 None 0 Human Binding pKi = 8.3 8.3 -2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77181 None 0 Human Binding pKi = 8.3 8.3 -2 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
44428745 92177 None 0 Human Binding pKi = 7.4 7.4 -6 5
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 635 23 2 6 7.9 COc1ccccc1CNCCCCCCN1CCC(CCC2CCN(CCCCCCNCc3ccccc3OC)CC2)CC1 10.1016/j.bmc.2007.01.022
CHEMBL242345 92177 None 0 Human Binding pKi = 7.4 7.4 -6 5
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M4 expressed in CHO cells
ChEMBL 635 23 2 6 7.9 COc1ccccc1CNCCCCCCN1CCC(CCC2CCN(CCCCCCNCc3ccccc3OC)CC2)CC1 10.1016/j.bmc.2007.01.022
164618698 188533 None 0 Human Binding pKi = 7.4 7.4 -43 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188533 None 0 Human Binding pKi = 7.4 7.4 -43 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188533 None 0 Human Binding pKi = 7.4 7.4 -43 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
11536903 2397 None 68 Human Binding pKi = 6.4 6.4 6 2
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
3262 2397 None 68 Human Binding pKi = 6.4 6.4 6 2
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
CHEMBL3770346 2397 None 68 Human Binding pKi = 6.4 6.4 6 2
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 311 3 2 5 2.7 COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 10.1039/C5MD00334B
57339144 92238 None 78 Human Binding pKi = 6.4 6.4 -5 6
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM4Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM4
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 10.6019/CHEMBL5212743
CHEMBL2426364 92238 None 78 Human Binding pKi = 6.4 6.4 -5 6
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM4Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM4
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 10.6019/CHEMBL5212743
73346332 92535 None 0 Human Binding pKi = 5.4 5.4 -2 4
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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 92535 None 0 Human Binding pKi = 5.4 5.4 -2 4
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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
107867 2974 None 55 Human Binding pKi = 6.4 6.4 -2 11
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
309 2974 None 55 Human Binding pKi = 6.4 6.4 -2 11
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
CHEMBL17045 2974 None 55 Human Binding pKi = 6.4 6.4 -2 11
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
21855 84246 None 42 Human Binding pKi = 6.4 6.4 -20 6
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
21855.0 84246 None 42 Human Binding pKi = 6.4 6.4 -20 6
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 84246 None 42 Human Binding pKi = 6.4 6.4 -20 6
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
DB08801 84246 None 42 Human Binding pKi = 6.4 6.4 -20 6
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
44593617 187431 None 0 Human Binding pKi = 6.4 6.4 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187431 None 0 Human Binding pKi = 6.4 6.4 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
162353382 181734 None 0 Human Binding pKi = 5.4 5.4 -4 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181734 None 0 Human Binding pKi = 5.4 5.4 -4 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
16086000 80356 None 0 Human Binding pKi = 7.4 7.4 -79 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 80356 None 0 Human Binding pKi = 7.4 7.4 -79 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
11766733 155754 None 0 Rat Binding pKi = 7.4 7.4 -208 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 155754 None 0 Rat Binding pKi = 7.4 7.4 -208 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 155754 None 0 Rat Binding pKi = 7.4 7.4 -208 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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
10421982 206041 None 0 Human Binding pKi = 6.4 6.4 -1 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
CHEMBL85190 206041 None 0 Human Binding pKi = 6.4 6.4 -1 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
56963799 74895 None 0 Human Binding pKi = 6.4 6.4 -1047 10
Binding affinity to human recombinant M4 receptorBinding affinity to human recombinant M4 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031737 74895 None 0 Human Binding pKi = 6.4 6.4 -1047 10
Binding affinity to human recombinant M4 receptorBinding affinity to human recombinant M4 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
155565286 176266 None 0 Human Binding pKi = 6.4 6.4 -1 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 18 6 8 2.7 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4579642 176266 None 0 Human Binding pKi = 6.4 6.4 -1 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 18 6 8 2.7 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595003 176266 None 0 Human Binding pKi = 6.4 6.4 -1 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 18 6 8 2.7 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
11012712 57829 None 2 Human Binding pKi = 5.4 5.4 -3 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 57829 None 2 Human Binding pKi = 5.4 5.4 -3 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
10969696 132105 None 0 Human Binding pKi = 5.4 5.4 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 132105 None 0 Human Binding pKi = 5.4 5.4 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
16086059 80775 None 0 Human Binding pKi = 7.4 7.4 -186 7
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 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 80775 None 0 Human Binding pKi = 7.4 7.4 -186 7
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 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
2284 3182 None 33 Human Binding pKi = 7.4 7.4 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3182 None 33 Human Binding pKi = 7.4 7.4 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3182 None 33 Human Binding pKi = 7.4 7.4 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3182 None 33 Human Binding pKi = 7.4 7.4 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3182 None 33 Human Binding pKi = 7.4 7.4 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
44318929 106862 None 0 Human Binding pKi = 7.4 7.4 2 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
CHEMBL314493 106862 None 0 Human Binding pKi = 7.4 7.4 2 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
16086059 80775 None 0 Human Binding pKi = 7.4 7.4 -186 7
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 80775 None 0 Human Binding pKi = 7.4 7.4 -186 7
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
44593618 187459 None 0 Human Binding pKi = 7.4 7.4 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187459 None 0 Human Binding pKi = 7.4 7.4 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
44439387 91717 None 0 Human Binding pKi = 4.4 4.4 -52 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 276 2 1 2 3.6 COc1cccc(C2=NCCc3c2[nH]c2ccccc32)c1 10.1016/j.bmcl.2007.01.093
CHEMBL240888 91717 None 0 Human Binding pKi = 4.4 4.4 -52 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 276 2 1 2 3.6 COc1cccc(C2=NCCc3c2[nH]c2ccccc32)c1 10.1016/j.bmcl.2007.01.093
164622017 188558 None 0 Human Binding pKi = 5.4 5.4 -47 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4871563 188558 None 0 Human Binding pKi = 5.4 5.4 -47 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028681 188558 None 0 Human Binding pKi = 5.4 5.4 -47 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
122387448 138308 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 299 3 2 5 2.6 CCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
CHEMBL3770968 138308 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 299 3 2 5 2.6 CCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
11006792 78922 None 0 Human Binding pKi = 7.4 7.4 -19 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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 78922 None 0 Human Binding pKi = 7.4 7.4 -19 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
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
137408738 191230 None 1 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]-NMS from human muscarinic acetylcholine M4 receptor expressed in CHO cell membrane by competitive binding assayDisplacement of [3H]-NMS from human muscarinic acetylcholine M4 receptor expressed in CHO cell membrane by competitive binding assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
CHEMBL5189893 191230 None 1 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]-NMS from human muscarinic acetylcholine M4 receptor expressed in CHO cell membrane by competitive binding assayDisplacement of [3H]-NMS from human muscarinic acetylcholine M4 receptor expressed in CHO cell membrane by competitive binding assay
ChEMBL 449 7 2 6 4.0 CC(=O)Nc1ccc(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)cc1 10.1016/j.bmcl.2021.128479
44517677 195435 None 0 Human Binding pKi = 5.4 5.4 -2 2
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 326 4 1 2 3.3 O=C(c1ccccc1C(F)(F)F)N(CC1CCC1)[C@H]1CCNC1 10.1016/j.bmcl.2009.06.096
CHEMBL552338 195435 None 0 Human Binding pKi = 5.4 5.4 -2 2
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 326 4 1 2 3.3 O=C(c1ccccc1C(F)(F)F)N(CC1CCC1)[C@H]1CCNC1 10.1016/j.bmcl.2009.06.096
122387448 138308 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 299 3 2 5 2.6 CCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
CHEMBL3770968 138308 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 299 3 2 5 2.6 CCNC(=O)c1sc2nc(OC)c(Cl)c(C)c2c1N 10.1039/C5MD00334B
10969390 59677 None 0 Human Binding pKi = 6.4 6.4 -60 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 59677 None 0 Human Binding pKi = 6.4 6.4 -60 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
145963288 161615 None 0 Human Binding pKi = 6.4 6.4 -2 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161615 None 0 Human Binding pKi = 6.4 6.4 -2 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
109018479 181818 None 1 Human Binding pKi = 5.4 5.4 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181818 None 1 Human Binding pKi = 5.4 5.4 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
24894630 188969 None 0 Human Binding pKi = 5.4 5.4 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 188969 None 0 Human Binding pKi = 5.4 5.4 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 188969 None 0 Human Binding pKi = 5.4 5.4 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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
24882532 95117 None 0 Rat Binding pKi = 6.4 6.4 -35 5
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 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 95117 None 0 Rat Binding pKi = 6.4 6.4 -35 5
Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M4 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
4189 206922 None 96 Human Binding pKi = 6.4 6.4 -10 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206922 None 96 Human Binding pKi = 6.4 6.4 -10 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206922 None 96 Human Binding pKi = 6.4 6.4 -10 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
118719926 115780 None 0 Human Binding pKi = 6.4 6.4 -102 8
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115780 None 0 Human Binding pKi = 6.4 6.4 -102 8
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
44593619 187460 None 0 Human Binding pKi = 6.4 6.4 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187460 None 0 Human Binding pKi = 6.4 6.4 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
46227457 14134 None 0 Human Binding pKi = 4.4 4.4 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14134 None 0 Human Binding pKi = 4.4 4.4 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14134 None 0 Human Binding pKi = 4.4 4.4 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
71454562 79654 None 0 Human Binding pKi = 7.4 7.4 -6 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 79654 None 0 Human Binding pKi = 7.4 7.4 -6 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
44318736 107021 None 0 Human Binding pKi = 6.4 6.4 -1 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
CHEMBL315428 107021 None 0 Human Binding pKi = 6.4 6.4 -1 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
44439409 91216 None 0 Human Binding pKi = 5.4 5.4 -44 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 322 5 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N(C)Cc3ccccc3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL240025 91216 None 0 Human Binding pKi = 5.4 5.4 -44 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 322 5 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N(C)Cc3ccccc3)cc21 10.1016/j.bmcl.2007.01.093
44439407 167415 None 0 Human Binding pKi = 5.4 5.4 -1 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 424 8 0 4 5.9 CCCCSC1CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL429644 167415 None 0 Human Binding pKi = 5.4 5.4 -1 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 424 8 0 4 5.9 CCCCSC1CCc2ccc(/N=C/N3CCc4cc(OC)c(OC)cc4C3)cc21 10.1016/j.bmcl.2007.01.093
124 2981 None 47 Human Binding pKi = 6.3 6.3 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2981 None 47 Human Binding pKi = 6.3 6.3 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2981 None 47 Human Binding pKi = 6.3 6.3 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636.0 2981 None 47 Human Binding pKi = 6.3 6.3 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2981 None 47 Human Binding pKi = 6.3 6.3 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2981 None 47 Human Binding pKi = 6.3 6.3 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
11834199 58771 None 0 Human Binding pKi = 6.3 6.3 -10 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 58771 None 0 Human Binding pKi = 6.3 6.3 -10 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
164614830 188500 None 0 Human Binding pKi = 5.3 5.3 -46 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4858774 188500 None 0 Human Binding pKi = 5.3 5.3 -46 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028275 188500 None 0 Human Binding pKi = 5.3 5.3 -46 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 889 20 10 13 -1.7 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44422697 11852 None 0 Human Binding pKi = 4.3 4.3 -8 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 11852 None 0 Human Binding pKi = 4.3 4.3 -8 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 11852 None 0 Human Binding pKi = 4.3 4.3 -8 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
44593624 188129 None 0 Human Binding pKi = 6.3 6.3 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 188129 None 0 Human Binding pKi = 6.3 6.3 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 188129 None 0 Human Binding pKi = 6.3 6.3 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
164623530 188573 None 0 Human Binding pKi = 5.3 5.3 -61 2
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4872632 188573 None 0 Human Binding pKi = 5.3 5.3 -61 2
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028763 188573 None 0 Human Binding pKi = 5.3 5.3 -61 2
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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](CCCNC(=N)N)NCCN1CCN(CC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44274417 98894 None 0 Human Binding pKi = 4.3 4.3 -5 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 98894 None 0 Human Binding pKi = 4.3 4.3 -5 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
11523051 96289 None 0 Human Binding pKi = 4.3 4.3 -3 5
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 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 96289 None 0 Human Binding pKi = 4.3 4.3 -3 5
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 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 96289 None 0 Human Binding pKi = 4.3 4.3 -3 5
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 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
11759058 120849 None 0 Human Binding pKi = 4.3 4.3 -1 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120849 None 0 Human Binding pKi = 4.3 4.3 -1 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
124087 1389 None 114 Human Binding pKi = 7.3 7.3 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
124087.0 1389 None 114 Human Binding pKi = 7.3 7.3 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1389 None 114 Human Binding pKi = 7.3 7.3 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1389 None 114 Human Binding pKi = 7.3 7.3 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1389 None 114 Human Binding pKi = 7.3 7.3 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1389 None 114 Human Binding pKi = 7.3 7.3 -7 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
71452382 83794 None 0 Human Binding pKi = 6.3 6.3 -14 10
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205812 83794 None 0 Human Binding pKi = 6.3 6.3 -14 10
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
44448538 12419 None 0 Human Binding pKi = 5.3 5.3 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12419 None 0 Human Binding pKi = 5.3 5.3 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12419 None 0 Human Binding pKi = 5.3 5.3 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
24894516 172708 None 0 Human Binding pKi = 4.3 4.3 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 172708 None 0 Human Binding pKi = 4.3 4.3 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@@H]2CCCN2C)o1 10.1021/jm800145d
44318736 107021 None 0 Human Binding pKi = 7.3 7.3 -1 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
CHEMBL315428 107021 None 0 Human Binding pKi = 7.3 7.3 -1 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
16086064 79960 None 0 Human Binding pKi = 7.3 7.3 -93 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 79960 None 0 Human Binding pKi = 7.3 7.3 -93 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
16086003 80431 None 0 Human Binding pKi = 6.3 6.3 -114 4
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 80431 None 0 Human Binding pKi = 6.3 6.3 -114 4
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
1212 1662 None 50 Human Binding pKi = 6.3 6.3 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1662 None 50 Human Binding pKi = 6.3 6.3 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1662 None 50 Human Binding pKi = 6.3 6.3 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372.0 1662 None 50 Human Binding pKi = 6.3 6.3 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1662 None 50 Human Binding pKi = 6.3 6.3 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1662 None 50 Human Binding pKi = 6.3 6.3 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL5277670 193943 None 0 Human Binding pKi = 8.3 8.3 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 930 19 2 5 13.0 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCN3CCC(OC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
3158 56267 None 27 Human Binding pKi = 8.2 8.2 -40 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
3158.0 56267 None 27 Human Binding pKi = 8.2 8.2 -40 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56267 None 27 Human Binding pKi = 8.2 8.2 -40 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
DB01142 56267 None 27 Human Binding pKi = 8.2 8.2 -40 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
10030021 169879 None 12 Human Binding pKi = 7.3 7.3 -6 5
Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M4 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 169879 None 12 Human Binding pKi = 7.3 7.3 -6 5
Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M4 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
10105296 205922 None 0 Human Binding pKi = 6.3 6.3 1 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
CHEMBL84113 205922 None 0 Human Binding pKi = 6.3 6.3 1 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
4746 204891 None 31 Human Binding pKi = 6.3 6.3 1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL1334033 204891 None 31 Human Binding pKi = 6.3 6.3 1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL75880 204891 None 31 Human Binding pKi = 6.3 6.3 1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
44439397 91212 None 0 Human Binding pKi = 4.3 4.3 -22 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 437 4 0 5 4.7 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)N(C(=O)OC(C)(C)C)CC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL240021 91212 None 0 Human Binding pKi = 4.3 4.3 -22 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 437 4 0 5 4.7 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)N(C(=O)OC(C)(C)C)CC3)CC2 10.1016/j.bmcl.2007.01.093
44593621 193297 None 0 Human Binding pKi = 6.3 6.3 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 193297 None 0 Human Binding pKi = 6.3 6.3 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
162353376 180427 None 0 Human Binding pKi = 4.3 4.3 -3 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 3 1 3 1.4 O=C(CCN1CCCc2ccccc21)N1CCC(O)C1 10.1016/j.bmcl.2020.127632
CHEMBL4752380 180427 None 0 Human Binding pKi = 4.3 4.3 -3 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 3 1 3 1.4 O=C(CCN1CCCc2ccccc21)N1CCC(O)C1 10.1016/j.bmcl.2020.127632
176 398 None 66 Human Binding pKi = 6.3 6.3 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pKi = 6.3 6.3 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
2157.0 398 None 66 Human Binding pKi = 6.3 6.3 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pKi = 6.3 6.3 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pKi = 6.3 6.3 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pKi = 6.3 6.3 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
1547484 940 None 74 Human Binding pKi = 6.3 6.3 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
1547484.0 940 None 74 Human Binding pKi = 6.3 6.3 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 940 None 74 Human Binding pKi = 6.3 6.3 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 940 None 74 Human Binding pKi = 6.3 6.3 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 940 None 74 Human Binding pKi = 6.3 6.3 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 940 None 74 Human Binding pKi = 6.3 6.3 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
44593616 193214 None 0 Human Binding pKi = 6.3 6.3 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 193214 None 0 Human Binding pKi = 6.3 6.3 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
145962050 161632 None 0 Human Binding pKi = 6.3 6.3 -2 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161632 None 0 Human Binding pKi = 6.3 6.3 -2 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
164625211 188588 None 0 Human Binding pKi = 5.3 5.3 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 20 9 12 -0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4869865 188588 None 0 Human Binding pKi = 5.3 5.3 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 20 9 12 -0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028864 188588 None 0 Human Binding pKi = 5.3 5.3 -15 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 20 9 12 -0.2 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
137635734 156112 None 0 Human Binding pKi = 5.3 5.3 -177 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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 156112 None 0 Human Binding pKi = 5.3 5.3 -177 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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
24894109 189028 None 0 Human Binding pKi = 5.3 5.3 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 189028 None 0 Human Binding pKi = 5.3 5.3 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 189028 None 0 Human Binding pKi = 5.3 5.3 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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
4715419 188741 None 34 Human Binding pKi = 4.3 4.3 -12 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc(C2CCCN2)o1 10.1021/jm800145d
CHEMBL505086 188741 None 34 Human Binding pKi = 4.3 4.3 -12 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc(C2CCCN2)o1 10.1021/jm800145d
71457691 83799 None 0 Human Binding pKi = 6.3 6.3 -1 10
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccccc1CN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205823 83799 None 0 Human Binding pKi = 6.3 6.3 -1 10
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccccc1CN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
1224 1432 None 83 Human Binding pKi = 7.3 7.3 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1432 None 83 Human Binding pKi = 7.3 7.3 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100.0 1432 None 83 Human Binding pKi = 7.3 7.3 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1432 None 83 Human Binding pKi = 7.3 7.3 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1432 None 83 Human Binding pKi = 7.3 7.3 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1432 None 83 Human Binding pKi = 7.3 7.3 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1432 None 83 Human Binding pKi = 7.3 7.3 -3 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
122387446 138276 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 355 3 2 5 2.9 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Br 10.1039/C5MD00334B
CHEMBL3770667 138276 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 355 3 2 5 2.9 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Br 10.1039/C5MD00334B
122387446 138276 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 355 3 2 5 2.9 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Br 10.1039/C5MD00334B
CHEMBL3770667 138276 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of AChDisplacement of [3H]NMS from human M4 mAChR expressed in FIpIn-CHO cells after 4 hrs by scintillation counting method in the presence of ACh
ChEMBL 355 3 2 5 2.9 COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Br 10.1039/C5MD00334B
162353374 180043 None 0 Human Binding pKi = 5.3 5.3 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180043 None 0 Human Binding pKi = 5.3 5.3 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
16086066 139235 None 0 Human Binding pKi = 7.3 7.3 -134 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 139235 None 0 Human Binding pKi = 7.3 7.3 -134 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
26987 949 None 33 Human Binding pKi = 7.3 7.3 -38 21
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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
26987.0 949 None 33 Human Binding pKi = 7.3 7.3 -38 21
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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 949 None 33 Human Binding pKi = 7.3 7.3 -38 21
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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
671 949 None 33 Human Binding pKi = 7.3 7.3 -38 21
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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 949 None 33 Human Binding pKi = 7.3 7.3 -38 21
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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 949 None 33 Human Binding pKi = 7.3 7.3 -38 21
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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
3168 9262 None 92 Human Binding pKi = 6.3 6.3 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
3168.0 9262 None 92 Human Binding pKi = 6.3 6.3 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9262 None 92 Human Binding pKi = 6.3 6.3 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
DB00450 9262 None 92 Human Binding pKi = 6.3 6.3 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
10418420 70273 None 0 Rat Binding pKi = 6.3 6.3 -40 4
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell 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 70273 None 0 Rat Binding pKi = 6.3 6.3 -40 4
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenatesInhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell 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
46227487 14127 None 0 Human Binding pKi = 4.3 4.3 -1 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14127 None 0 Human Binding pKi = 4.3 4.3 -1 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14127 None 0 Human Binding pKi = 4.3 4.3 -1 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
24841480 183899 None 0 Human Binding pKi = 7.3 7.3 -26 20
Antagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M4 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 183899 None 0 Human Binding pKi = 7.3 7.3 -26 20
Antagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
44627854 197709 None 0 Human Binding pKi = 7.3 7.3 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 197709 None 0 Human Binding pKi = 7.3 7.3 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
44437256 12396 None 0 Human Binding pKi = 5.3 5.3 -1 4
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 12396 None 0 Human Binding pKi = 5.3 5.3 -1 4
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 12396 None 0 Human Binding pKi = 5.3 5.3 -1 4
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 282 4 0 4 2.8 C(#CCN1CCCC1)COc1cc(-c2ccccc2)on1 10.1016/j.bmc.2007.09.003
44627855 197371 None 0 Human Binding pKi = 6.3 6.3 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 197371 None 0 Human Binding pKi = 6.3 6.3 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
3652 46244 None 70 Human Binding pKi = 5.3 5.3 -1 9
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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 46244 None 70 Human Binding pKi = 5.3 5.3 -1 9
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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
10066369 120258 None 0 Human Binding pKi = 5.3 5.3 -22 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120258 None 0 Human Binding pKi = 5.3 5.3 -22 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
44274432 80127 None 0 Human Binding pKi = 4.3 4.3 -3 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 80127 None 0 Human Binding pKi = 4.3 4.3 -3 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
103 4153 None 61 Human Binding pKi = 6.3 6.3 -190 53
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
2875 4153 None 61 Human Binding pKi = 6.3 6.3 -190 53
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
5736 4153 None 61 Human Binding pKi = 6.3 6.3 -190 53
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
CHEMBL285802 4153 None 61 Human Binding pKi = 6.3 6.3 -190 53
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
DB09225 4153 None 61 Human Binding pKi = 6.3 6.3 -190 53
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
5318 15576 None 49 Human Binding pKi = 6.3 6.3 1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15576 None 49 Human Binding pKi = 6.3 6.3 1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15576 None 49 Human Binding pKi = 6.3 6.3 1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
155548586 176597 None 0 Human Binding pKi = 7.3 7.3 -10 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176597 None 0 Human Binding pKi = 7.3 7.3 -10 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176597 None 0 Human Binding pKi = 7.3 7.3 -10 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
156016047 178260 None 0 Human Binding pKi = 5.3 5.3 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178260 None 0 Human Binding pKi = 5.3 5.3 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178260 None 0 Human Binding pKi = 5.3 5.3 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
24894514 172734 None 3 Human Binding pKi = 4.3 4.3 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@H]1c1ccco1 10.1021/jm800145d
CHEMBL450729 172734 None 3 Human Binding pKi = 4.3 4.3 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@H]1c1ccco1 10.1021/jm800145d
14537188 136546 None 0 Human Binding pKi = 6.3 6.3 -173 5
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 136546 None 0 Human Binding pKi = 6.3 6.3 -173 5
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
155543345 176686 None 0 Human Binding pKi = 7.2 7.2 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176686 None 0 Human Binding pKi = 7.2 7.2 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176686 None 0 Human Binding pKi = 7.2 7.2 -6 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
71575652 86198 None 0 Human Binding pKi = 5.2 5.2 -10 5
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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 86198 None 0 Human Binding pKi = 5.2 5.2 -10 5
Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M4 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
137645938 157583 None 0 Human Binding pKi = 6.2 6.2 -416 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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 157583 None 0 Human Binding pKi = 6.2 6.2 -416 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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
2719 917 None 74 Human Binding pKi = 5.2 5.2 -5 11
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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 917 None 74 Human Binding pKi = 5.2 5.2 -5 11
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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
607 917 None 74 Human Binding pKi = 5.2 5.2 -5 11
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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 917 None 74 Human Binding pKi = 5.2 5.2 -5 11
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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 917 None 74 Human Binding pKi = 5.2 5.2 -5 11
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) 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
162353379 180962 None 0 Human Binding pKi = 5.2 5.2 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180962 None 0 Human Binding pKi = 5.2 5.2 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
46227461 14136 None 0 Human Binding pKi = 4.2 4.2 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14136 None 0 Human Binding pKi = 4.2 4.2 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14136 None 0 Human Binding pKi = 4.2 4.2 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
4011 82408 None 49 Human Binding pKi = 7.2 7.2 -11 24
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82408 None 49 Human Binding pKi = 7.2 7.2 -11 24
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
164620270 188542 None 0 Human Binding pKi = 7.2 7.2 -50 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188542 None 0 Human Binding pKi = 7.2 7.2 -50 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188542 None 0 Human Binding pKi = 7.2 7.2 -50 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
44593625 188130 None 0 Human Binding pKi = 7.2 7.2 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 188130 None 0 Human Binding pKi = 7.2 7.2 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 188130 None 0 Human Binding pKi = 7.2 7.2 -5 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
156015971 178282 None 0 Human Binding pKi = 7.2 7.2 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178282 None 0 Human Binding pKi = 7.2 7.2 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178282 None 0 Human Binding pKi = 7.2 7.2 -3 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
164627575 188608 None 0 Human Binding pKi = 6.2 6.2 -33 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 859 21 8 11 1.4 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4873979 188608 None 0 Human Binding pKi = 6.2 6.2 -33 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 859 21 8 11 1.4 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5029004 188608 None 0 Human Binding pKi = 6.2 6.2 -33 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 859 21 8 11 1.4 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
118719925 115779 None 0 Human Binding pKi = 6.2 6.2 -7 8
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115779 None 0 Human Binding pKi = 6.2 6.2 -7 8
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
162353381 180029 None 0 Human Binding pKi = 4.2 4.2 -52 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 287 4 1 4 2.9 O=C(CCN1CCCc2ccccc21)Nc1nccs1 10.1016/j.bmcl.2020.127632
CHEMBL4747438 180029 None 0 Human Binding pKi = 4.2 4.2 -52 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 287 4 1 4 2.9 O=C(CCN1CCCc2ccccc21)Nc1nccs1 10.1016/j.bmcl.2020.127632
162353380 182494 None 0 Human Binding pKi = 4.2 4.2 -1 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 182494 None 0 Human Binding pKi = 4.2 4.2 -1 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
24894633 176900 None 0 Human Binding pKi = 4.2 4.2 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 176900 None 0 Human Binding pKi = 4.2 4.2 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@H]2CCCN2C)o1 10.1021/jm800145d
9843967 155458 None 1 Human Binding pKi = 6.2 6.2 -1 2
Binding ability of compound to m4 muscarinic receptorBinding ability of compound to m4 muscarinic receptor
ChEMBL 400 7 1 5 3.4 Nc1cccc(-c2ccc(CCN3CCN(CC(=O)c4ccccc4)CC3)cc2)n1 10.1016/s0960-894x(99)00432-1
CHEMBL40391 155458 None 1 Human Binding pKi = 6.2 6.2 -1 2
Binding ability of compound to m4 muscarinic receptorBinding ability of compound to m4 muscarinic receptor
ChEMBL 400 7 1 5 3.4 Nc1cccc(-c2ccc(CCN3CCN(CC(=O)c4ccccc4)CC3)cc2)n1 10.1016/s0960-894x(99)00432-1
137645406 157902 None 0 Human Binding pKi = 6.2 6.2 -74 13
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 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 157902 None 0 Human Binding pKi = 6.2 6.2 -74 13
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M4 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
73355420 92551 None 0 Human Binding pKi = 5.2 5.2 -2 2
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 355 6 0 4 3.3 COc1cc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432061 92551 None 0 Human Binding pKi = 5.2 5.2 -2 2
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 355 6 0 4 3.3 COc1cc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
44437249 11872 None 0 Human Binding pKi = 5.2 5.2 -2 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 11872 None 0 Human Binding pKi = 5.2 5.2 -2 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 11872 None 0 Human Binding pKi = 5.2 5.2 -2 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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
44437259 11879 None 0 Human Binding pKi = 5.2 5.2 -4 4
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 11879 None 0 Human Binding pKi = 5.2 5.2 -4 4
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 11879 None 0 Human Binding pKi = 5.2 5.2 -4 4
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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
13567081 11234 None 0 Human Binding pKi = 8.2 8.2 -5 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 11234 None 0 Human Binding pKi = 8.2 8.2 -5 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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 11234 None 0 Human Binding pKi = 8.2 8.2 -5 5
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 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
44455198 97657 None 0 Human Binding pKi = 8.2 8.2 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 97657 None 0 Human Binding pKi = 8.2 8.2 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 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 97657 None 0 Rat Binding pKi = 8.2 8.2 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 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 97657 None 0 Rat Binding pKi = 8.2 8.2 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 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
135398737 958 None 93 Human Binding pKi = 8.2 8.2 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
135398737.0 958 None 93 Human Binding pKi = 8.2 8.2 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 None 93 Human Binding pKi = 8.2 8.2 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 None 93 Human Binding pKi = 8.2 8.2 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 None 93 Human Binding pKi = 8.2 8.2 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 None 93 Human Binding pKi = 8.2 8.2 -7 89
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
132947 3864 None 9 Human Binding pKi = 8.2 8.2 -22 9
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 3864 None 9 Human Binding pKi = 8.2 8.2 -22 9
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 3864 None 9 Human Binding pKi = 8.2 8.2 -22 9
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 170406 None 0 Human Binding pKi = 8.2 8.2 -23 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 3 hrs by beta counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 170406 None 0 Human Binding pKi = 8.2 8.2 -23 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 3 hrs by beta counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
129989 451 None 51 Human Binding pKi = 8.2 8.2 -1 9
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 451 None 51 Human Binding pKi = 8.2 8.2 -1 9
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 451 None 51 Human Binding pKi = 8.2 8.2 -1 9
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
11498 3019 None 41 Human Binding pKi = 8.2 8.2 38 6
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 3019 None 41 Human Binding pKi = 8.2 8.2 38 6
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 3019 None 41 Human Binding pKi = 8.2 8.2 38 6
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
152278786 182752 None 1 Human Binding pKi = 8.2 8.2 -7 3
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 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 M4 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 182752 None 1 Human Binding pKi = 8.2 8.2 -7 3
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 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 M4 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
118719923 115777 None 0 Human Binding pKi = 8.2 8.2 1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115777 None 0 Human Binding pKi = 8.2 8.2 1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
44386115 131438 None 0 Human Binding pKi = 7.2 7.2 -28 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 650 16 3 4 6.2 O=C(CCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL369062 131438 None 0 Human Binding pKi = 7.2 7.2 -28 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 650 16 3 4 6.2 O=C(CCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
2230 465 None 60 Human Binding pKi = 4.2 4.2 -218 10
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
296 465 None 60 Human Binding pKi = 4.2 4.2 -218 10
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
CHEMBL7303 465 None 60 Human Binding pKi = 4.2 4.2 -218 10
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
DB04365 465 None 60 Human Binding pKi = 4.2 4.2 -218 10
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
11808947 59453 None 0 Human Binding pKi = 6.2 6.2 -11 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 59453 None 0 Human Binding pKi = 6.2 6.2 -11 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
44593627 193299 None 0 Human Binding pKi = 6.2 6.2 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 193299 None 0 Human Binding pKi = 6.2 6.2 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 193299 None 0 Human Binding pKi = 6.2 6.2 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
44437295 11893 None 0 Human Binding pKi = 5.2 5.2 -6 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
CHEMBL1182472 11893 None 0 Human Binding pKi = 5.2 5.2 -6 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
CHEMBL239866 11893 None 0 Human Binding pKi = 5.2 5.2 -6 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
9894173 15150 None 4 Human Binding pKi = 7.2 7.2 -69 5
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 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 15150 None 4 Human Binding pKi = 7.2 7.2 -69 5
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 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
155522355 176409 None 0 Human Binding pKi = 7.2 7.2 -47 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176409 None 0 Human Binding pKi = 7.2 7.2 -47 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176409 None 0 Human Binding pKi = 7.2 7.2 -47 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
135430667 4958 None 0 Human Binding pKi = 7.2 7.2 35 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 4958 None 0 Human Binding pKi = 7.2 7.2 35 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
9968046 198163 None 0 Human Binding pKi = 6.2 6.2 -3 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 198163 None 0 Human Binding pKi = 6.2 6.2 -3 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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
11045444 59189 None 0 Human Binding pKi = 6.2 6.2 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 59189 None 0 Human Binding pKi = 6.2 6.2 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
44448417 11909 None 0 Human Binding pKi = 6.2 6.2 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11909 None 0 Human Binding pKi = 6.2 6.2 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11909 None 0 Human Binding pKi = 6.2 6.2 1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
66561966 74703 None 0 Human Binding pKi = 5.2 5.2 -2 4
Inhibition of M4 muscarinic receptorInhibition of M4 muscarinic receptor
ChEMBL 193 2 0 1 3.2 C1CCC(CN2C3CCC2CC3)CC1 10.1016/j.bmcl.2012.04.077
CHEMBL2030625 74703 None 0 Human Binding pKi = 5.2 5.2 -2 4
Inhibition of M4 muscarinic receptorInhibition of M4 muscarinic receptor
ChEMBL 193 2 0 1 3.2 C1CCC(CN2C3CCC2CC3)CC1 10.1016/j.bmcl.2012.04.077
73346336 92545 None 0 Human Binding pKi = 6.2 6.2 -1 6
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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 92545 None 0 Human Binding pKi = 6.2 6.2 -1 6
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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
71128 96810 None 25 Human Binding pKi = 6.2 6.2 -30 7
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 96810 None 25 Human Binding pKi = 6.2 6.2 -30 7
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
155522355 176409 None 0 Human Binding pKi = 7.2 7.2 -47 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 176409 None 0 Human Binding pKi = 7.2 7.2 -47 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 176409 None 0 Human Binding pKi = 7.2 7.2 -47 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
10770914 25061 None 0 Rat Binding pKi = 7.2 7.2 -213 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 691 25 3 7 6.4 CN(CCCCCCCCN(C)C(=O)CCCCCNCCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
CHEMBL134692 25061 None 0 Rat Binding pKi = 7.2 7.2 -213 5
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
ChEMBL 691 25 3 7 6.4 CN(CCCCCCCCN(C)C(=O)CCCCCNCCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
16094783 136567 None 0 Human Binding pKi = 7.2 7.2 -1 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL373888 136567 None 0 Human Binding pKi = 7.2 7.2 -1 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
164621443 188554 None 0 Human Binding pKi = 6.2 6.2 -37 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 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(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4867483 188554 None 0 Human Binding pKi = 6.2 6.2 -37 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 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(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028653 188554 None 0 Human Binding pKi = 6.2 6.2 -37 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 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(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
2551 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
2551.0 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
298 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
488 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
CHEMBL965 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
DB00411 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
164622564 188561 None 0 Human Binding pKi = 5.2 5.2 -25 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4862221 188561 None 0 Human Binding pKi = 5.2 5.2 -25 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028706 188561 None 0 Human Binding pKi = 5.2 5.2 -25 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 21 9 12 0.2 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
162353371 181650 None 0 Human Binding pKi = 5.2 5.2 -2 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 2 0 2 2.5 CC1CCc2ccccc2N1CC(=O)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4775999 181650 None 0 Human Binding pKi = 5.2 5.2 -2 3
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 2 0 2 2.5 CC1CCc2ccccc2N1CC(=O)N1CCCC1 10.1016/j.bmcl.2020.127632
2551 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
2551.0 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
298 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
488 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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
2551.0 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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
298 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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
488 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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
300 2510 None 15 Human Binding pKi = 5.2 5.2 -3 6
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 2510 None 15 Human Binding pKi = 5.2 5.2 -3 6
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 2510 None 15 Human Binding pKi = 5.2 5.2 -3 6
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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
2551 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
2551.0 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
298 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
488 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
2551.0 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
298 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
488 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 794 None 23 Human Binding pKi = 5.2 5.2 -21 11
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
156010398 178236 None 0 Human Binding pKi = 5.2 5.2 -31 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178236 None 0 Human Binding pKi = 5.2 5.2 -31 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178236 None 0 Human Binding pKi = 5.2 5.2 -31 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
657255 199084 None 34 Human Binding pKi = 6.2 6.2 -9 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 199084 None 34 Human Binding pKi = 6.2 6.2 -9 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
44627744 14040 None 0 Human Binding pKi = 7.2 7.2 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14040 None 0 Human Binding pKi = 7.2 7.2 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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 14040 None 0 Human Binding pKi = 7.2 7.2 -2 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 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
11034265 120373 None 0 Human Binding pKi = 6.2 6.2 -5 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120373 None 0 Human Binding pKi = 6.2 6.2 -5 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
162353393 179439 None 0 Human Binding pKi = 5.2 5.2 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 179439 None 0 Human Binding pKi = 5.2 5.2 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
24894628 179123 None 0 Human Binding pKi = 5.2 5.2 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 179123 None 0 Human Binding pKi = 5.2 5.2 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 179123 None 0 Human Binding pKi = 5.2 5.2 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCCC1c1ccco1 10.1021/jm800145d
15157139 99811 None 0 Human Binding pKi = 7.2 7.2 -2 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 331 8 0 3 4.4 CN(C)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL285440 99811 None 0 Human Binding pKi = 7.2 7.2 -2 4
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 331 8 0 3 4.4 CN(C)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
73353884 92322 None 0 Human Binding pKi = 5.2 5.2 -5 8
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2429890 92322 None 0 Human Binding pKi = 5.2 5.2 -5 8
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
71463063 83801 None 0 Human Binding pKi = 6.2 6.2 -1 8
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205825 83801 None 0 Human Binding pKi = 6.2 6.2 -1 8
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
44318851 104726 None 0 Human Binding pKi = 6.2 6.2 -1 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL310558 104726 None 0 Human Binding pKi = 6.2 6.2 -1 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
11808946 120636 None 0 Human Binding pKi = 6.2 6.2 -6 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120636 None 0 Human Binding pKi = 6.2 6.2 -6 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
25147647 182139 None 0 Human Binding pKi = 5.2 5.2 -6 3
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 405 2 1 5 2.9 CN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)[C@@H]2CCCC[C@H]21 10.1016/j.bmc.2008.06.025
CHEMBL478226 182139 None 0 Human Binding pKi = 5.2 5.2 -6 3
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells
ChEMBL 405 2 1 5 2.9 CN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)[C@@H]2CCCC[C@H]21 10.1016/j.bmc.2008.06.025
156009698 178336 None 0 Human Binding pKi = 7.2 7.2 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178336 None 0 Human Binding pKi = 7.2 7.2 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178336 None 0 Human Binding pKi = 7.2 7.2 -1 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
11015312 5274 None 0 Human Binding pKi = 7.2 7.2 15 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5274 None 0 Human Binding pKi = 7.2 7.2 15 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 420 5 1 5 4.9 CCCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
1016 3747 None 78 Human Binding pKi = 6.2 6.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pKi = 6.2 6.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pKi = 6.2 6.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pKi = 6.2 6.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pKi = 6.2 6.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pKi = 6.2 6.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
422063 196077 None 2 Human Binding pKi = 6.2 6.2 -4 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 196077 None 2 Human Binding pKi = 6.2 6.2 -4 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 196077 None 2 Human Binding pKi = 6.2 6.2 -4 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
44439394 145122 None 0 Human Binding pKi = 4.2 4.2 -398 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 308 3 2 2 4.3 CSc1ccc(CC2NCCc3c2[nH]c2ccccc32)cc1 10.1016/j.bmcl.2007.01.093
CHEMBL391191 145122 None 0 Human Binding pKi = 4.2 4.2 -398 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 308 3 2 2 4.3 CSc1ccc(CC2NCCc3c2[nH]c2ccccc32)cc1 10.1016/j.bmcl.2007.01.093
73355418 92546 None 0 Human Binding pKi = 5.2 5.2 -6 3
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 3 3.3 COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432056 92546 None 0 Human Binding pKi = 5.2 5.2 -6 3
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 3 3.3 COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
24809738 11889 None 0 Human Binding pKi = 6.2 6.2 -13 4
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 11889 None 0 Human Binding pKi = 6.2 6.2 -13 4
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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 11889 None 0 Human Binding pKi = 6.2 6.2 -13 4
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 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
71450550 83807 None 0 Human Binding pKi = 6.2 6.2 -1 16
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 83807 None 0 Human Binding pKi = 6.2 6.2 -1 16
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
164609302 188463 None 0 Human Binding pKi = 7.2 7.2 -36 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4846958 188463 None 0 Human Binding pKi = 7.2 7.2 -36 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5027951 188463 None 0 Human Binding pKi = 7.2 7.2 -36 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 704 17 8 9 1.5 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](CCNC(=N)N)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
44207909 16699 None 3 Human Binding pKi = 5.2 5.2 -26 9
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 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 16699 None 3 Human Binding pKi = 5.2 5.2 -26 9
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
44422699 11851 None 0 Human Binding pKi = 4.2 4.2 -10 4
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 11851 None 0 Human Binding pKi = 4.2 4.2 -10 4
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 11851 None 0 Human Binding pKi = 4.2 4.2 -10 4
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
24894631 176764 None 3 Human Binding pKi = 4.2 4.2 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCCC1c1ccco1 10.1021/jm800145d
CHEMBL460470 176764 None 3 Human Binding pKi = 4.2 4.2 -2 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCCC1c1ccco1 10.1021/jm800145d
73355416 92537 None 0 Human Binding pKi = 5.2 5.2 1 2
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 0 3 1.8 CN(Cc1cccnc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432043 92537 None 0 Human Binding pKi = 5.2 5.2 1 2
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 0 3 1.8 CN(Cc1cccnc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
11498 3019 None 41 Human Binding pKi = 8.2 8.2 38 6
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 3019 None 41 Human Binding pKi = 8.2 8.2 38 6
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 3019 None 41 Human Binding pKi = 8.2 8.2 38 6
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1021/jm011116o
11143997 5022 None 0 Human Binding pKi = 8.2 8.2 32 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5022 None 0 Human Binding pKi = 8.2 8.2 32 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
ChEMBL 408 3 1 5 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
315401 89812 None 4 Human Binding pKi = 8.1 8.1 -5 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 89812 None 4 Human Binding pKi = 8.1 8.1 -5 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
71128 96810 None 25 Human Binding pKi = 8.1 8.1 -30 7
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00085a017
CHEMBL26505 96810 None 25 Human Binding pKi = 8.1 8.1 -30 7
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M4 subtype
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00085a017
164621305 188552 None 0 Human Binding pKi = 8.1 8.1 -29 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
CHEMBL4863285 188552 None 0 Human Binding pKi = 8.1 8.1 -29 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
CHEMBL5028642 188552 None 0 Human Binding pKi = 8.1 8.1 -29 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
164617895 188525 None 0 Human Binding pKi = 8.1 8.1 -41 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188525 None 0 Human Binding pKi = 8.1 8.1 -41 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188525 None 0 Human Binding pKi = 8.1 8.1 -41 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
137638270 156877 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
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 156877 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranesDisplacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes
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
129989 451 None 51 Human Binding pKi = 8.1 8.1 -1 9
Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M4 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 451 None 51 Human Binding pKi = 8.1 8.1 -1 9
Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M4 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 451 None 51 Human Binding pKi = 8.1 8.1 -1 9
Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M4 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
118719921 115774 None 0 Human Binding pKi = 8.1 8.1 -1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115774 None 0 Human Binding pKi = 8.1 8.1 -1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
57326325 77184 None 0 Human Binding pKi = 7.2 7.2 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77184 None 0 Human Binding pKi = 7.2 7.2 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 77184 None 0 Human Binding pKi = 7.2 7.2 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
156014205 178292 None 0 Human Binding pKi = 7.2 7.2 -7 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178292 None 0 Human Binding pKi = 7.2 7.2 -7 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178292 None 0 Human Binding pKi = 7.2 7.2 -7 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
57326325 77184 None 0 Human Binding pKi = 7.2 7.2 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 77184 None 0 Human Binding pKi = 7.2 7.2 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 77184 None 0 Human Binding pKi = 7.2 7.2 -1 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
44439405 91812 None 0 Human Binding pKi = 6.2 6.2 -2 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 440 4 0 5 5.3 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C1SCCSC1CC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL241282 91812 None 0 Human Binding pKi = 6.2 6.2 -2 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 440 4 0 5 5.3 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C1SCCSC1CC3)CC2 10.1016/j.bmcl.2007.01.093
44318930 106172 None 0 Human Binding pKi = 6.2 6.2 2 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
CHEMBL313738 106172 None 0 Human Binding pKi = 6.2 6.2 2 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
44439389 91780 None 0 Human Binding pKi = 4.2 4.2 -8 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 324 3 1 5 2.8 COc1ccc2[nH]c3c(c2c1)CCN=C3c1cc([N+](=O)[O-])cn1C 10.1016/j.bmcl.2007.01.093
CHEMBL241099 91780 None 0 Human Binding pKi = 4.2 4.2 -8 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 324 3 1 5 2.8 COc1ccc2[nH]c3c(c2c1)CCN=C3c1cc([N+](=O)[O-])cn1C 10.1016/j.bmcl.2007.01.093
53324553 56855 None 0 Human Binding pKi = 6.2 6.2 1 10
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL1643900 56855 None 0 Human Binding pKi = 6.2 6.2 1 10
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
53324553 56855 None 0 Human Binding pKi = 6.2 6.2 1 10
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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 56855 None 0 Human Binding pKi = 6.2 6.2 1 10
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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
73352414 92532 None 0 Human Binding pKi = 6.2 6.2 1 5
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 257 3 1 1 3.3 C1CCC(CN[C@H]2C3C4CC5C6C4CC3C6C52)CC1 10.1016/j.bmc.2013.07.045
CHEMBL2432038 92532 None 0 Human Binding pKi = 6.2 6.2 1 5
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 257 3 1 1 3.3 C1CCC(CN[C@H]2C3C4CC5C6C4CC3C6C52)CC1 10.1016/j.bmc.2013.07.045
164613685 188489 None 0 Human Binding pKi = 6.2 6.2 -36 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 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(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4861655 188489 None 0 Human Binding pKi = 6.2 6.2 -36 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 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(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028207 188489 None 0 Human Binding pKi = 6.2 6.2 -36 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 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(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
164617650 188521 None 0 Human Binding pKi = 5.2 5.2 -5 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 676 13 8 9 -0.1 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4860171 188521 None 0 Human Binding pKi = 5.2 5.2 -5 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 676 13 8 9 -0.1 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028445 188521 None 0 Human Binding pKi = 5.2 5.2 -5 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 676 13 8 9 -0.1 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
3652 4097 None 79 Human Binding pKi = 7.1 7.1 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 4097 None 79 Human Binding pKi = 7.1 7.1 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 4097 None 79 Human Binding pKi = 7.1 7.1 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809.0 4097 None 79 Human Binding pKi = 7.1 7.1 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 4097 None 79 Human Binding pKi = 7.1 7.1 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 4097 None 79 Human Binding pKi = 7.1 7.1 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
11092603 4861 None 0 Human Binding pKi = 7.1 7.1 2 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 4861 None 0 Human Binding pKi = 7.1 7.1 2 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
10874119 4907 None 0 Human Binding pKi = 7.1 7.1 15 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 4907 None 0 Human Binding pKi = 7.1 7.1 15 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
164620290 188543 None 0 Human Binding pKi = 6.1 6.1 -15 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 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(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4870729 188543 None 0 Human Binding pKi = 6.1 6.1 -15 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 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(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028589 188543 None 0 Human Binding pKi = 6.1 6.1 -15 4
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 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(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
137640201 156961 None 2 Human Binding pKi = 6.1 6.1 -575 13
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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 156961 None 2 Human Binding pKi = 6.1 6.1 -575 13
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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
162353372 181387 None 0 Human Binding pKi = 5.1 5.1 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181387 None 0 Human Binding pKi = 5.1 5.1 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
156014875 178241 None 0 Human Binding pKi = 5.1 5.1 -5 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178241 None 0 Human Binding pKi = 5.1 5.1 -5 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178241 None 0 Human Binding pKi = 5.1 5.1 -5 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
73350932 92536 None 0 Human Binding pKi = 5.1 5.1 - 1
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 339 5 0 4 2.5 COc1ccc(CN(C)[C@H]2C3C4CC5C3C(=O)C3C5C4C32)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432042 92536 None 0 Human Binding pKi = 5.1 5.1 - 1
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
ChEMBL 339 5 0 4 2.5 COc1ccc(CN(C)[C@H]2C3C4CC5C3C(=O)C3C5C4C32)cc1OC 10.1016/j.bmc.2013.07.045
44385809 61466 None 0 Human Binding pKi = 7.1 7.1 -22 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 636 15 3 4 5.8 O=C(CCCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL177040 61466 None 0 Human Binding pKi = 7.1 7.1 -22 5
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 636 15 3 4 5.8 O=C(CCCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
44448421 12337 None 0 Human Binding pKi = 7.1 7.1 9 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12337 None 0 Human Binding pKi = 7.1 7.1 9 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 12337 None 0 Human Binding pKi = 7.1 7.1 9 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
10925451 58772 None 0 Human Binding pKi = 6.1 6.1 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 58772 None 0 Human Binding pKi = 6.1 6.1 -2 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
10066369 120258 None 0 Human Binding pKi = 6.1 6.1 -22 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120258 None 0 Human Binding pKi = 6.1 6.1 -22 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
11011332 120802 None 1 Human Binding pKi = 5.1 5.1 -1 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120802 None 1 Human Binding pKi = 5.1 5.1 -1 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
108993439 179860 None 1 Human Binding pKi = 4.1 4.1 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 179860 None 1 Human Binding pKi = 4.1 4.1 -3 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
49783209 17609 None 0 Human Binding pKi = 6.1 6.1 -380 26
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17609 None 0 Human Binding pKi = 6.1 6.1 -380 26
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
2551 794 None 23 Human Binding pKi = 5.1 5.1 -21 11
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
2551.0 794 None 23 Human Binding pKi = 5.1 5.1 -21 11
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
298 794 None 23 Human Binding pKi = 5.1 5.1 -21 11
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
488 794 None 23 Human Binding pKi = 5.1 5.1 -21 11
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
CHEMBL965 794 None 23 Human Binding pKi = 5.1 5.1 -21 11
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
DB00411 794 None 23 Human Binding pKi = 5.1 5.1 -21 11
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
44627742 198377 None 0 Human Binding pKi = 7.1 7.1 -5 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 323 4 0 2 5.8 CN1CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL576707 198377 None 0 Human Binding pKi = 7.1 7.1 -5 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells by scintillation counting
ChEMBL 323 4 0 2 5.8 CN1CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
109032820 182875 None 1 Human Binding pKi = 6.1 6.1 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 182875 None 1 Human Binding pKi = 6.1 6.1 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
44439388 91773 None 0 Human Binding pKi = 4.1 4.1 -22 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 306 3 1 3 3.6 COc1cccc(C2=NCCc3c2[nH]c2ccc(OC)cc32)c1 10.1016/j.bmcl.2007.01.093
CHEMBL241082 91773 None 0 Human Binding pKi = 4.1 4.1 -22 3
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 306 3 1 3 3.6 COc1cccc(C2=NCCc3c2[nH]c2ccc(OC)cc32)c1 10.1016/j.bmcl.2007.01.093
12488 1657 None 56 Human Binding pKi = 6.1 6.1 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 1657 None 56 Human Binding pKi = 6.1 6.1 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 1657 None 56 Human Binding pKi = 6.1 6.1 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 1657 None 56 Human Binding pKi = 6.1 6.1 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10226457 12975 None 0 Human Binding pKi = 7.1 7.1 -19 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL1189471 12975 None 0 Human Binding pKi = 7.1 7.1 -19 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL538793 12975 None 0 Human Binding pKi = 7.1 7.1 -19 5
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
155525065 176554 None 0 Human Binding pKi = 7.1 7.1 -3 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176554 None 0 Human Binding pKi = 7.1 7.1 -3 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176554 None 0 Human Binding pKi = 7.1 7.1 -3 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
16094791 83257 None 0 Human Binding pKi = 7.1 7.1 -1 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL218755 83257 None 0 Human Binding pKi = 7.1 7.1 -1 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
44304818 203306 None 0 Rat Binding pKi = 5.1 5.1 -30 7
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64788 203306 None 0 Rat Binding pKi = 5.1 5.1 -30 7
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
44304818 203306 None 0 Human Binding pKi = 5.1 5.1 -30 7
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64788 203306 None 0 Human Binding pKi = 5.1 5.1 -30 7
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
44437270 12328 None 0 Human Binding pKi = 6.1 6.1 -19 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL1185211 12328 None 0 Human Binding pKi = 6.1 6.1 -19 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL398043 12328 None 0 Human Binding pKi = 6.1 6.1 -19 5
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
44299564 199087 None 0 Human Binding pKi = 6.1 6.1 -1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 199087 None 0 Human Binding pKi = 6.1 6.1 -1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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
10109893 82165 None 0 Human Binding pKi = 6.1 6.1 -2 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
CHEMBL216983 82165 None 0 Human Binding pKi = 6.1 6.1 -2 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
CHEMBL544840 82165 None 0 Human Binding pKi = 6.1 6.1 -2 5
Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
156012563 178248 None 0 Human Binding pKi = 5.1 5.1 -3 4
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178248 None 0 Human Binding pKi = 5.1 5.1 -3 4
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178248 None 0 Human Binding pKi = 5.1 5.1 -3 4
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
24894515 176870 None 4 Human Binding pKi = 4.1 4.1 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@@H]1c1ccco1 10.1021/jm800145d
CHEMBL461502 176870 None 4 Human Binding pKi = 4.1 4.1 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@@H]1c1ccco1 10.1021/jm800145d
4841 67427 None 5 Human Binding pKi = 8.1 8.1 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 67427 None 5 Human Binding pKi = 8.1 8.1 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 67427 None 5 Human Binding pKi = 8.1 8.1 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
319 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
321 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
444031 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
444031.0 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
784 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
CHEMBL1346 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
DB00496 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
324 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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
10660 14416 None 58 Human Binding pKi = 7.1 7.1 -2 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
10660.0 14416 None 58 Human Binding pKi = 7.1 7.1 -2 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
441281.0 14416 None 58 Human Binding pKi = 7.1 7.1 -2 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14416 None 58 Human Binding pKi = 7.1 7.1 -2 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
DB00985 14416 None 58 Human Binding pKi = 7.1 7.1 -2 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
11748799 165411 None 0 Human Binding pKi = 7.1 7.1 -5 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 165411 None 0 Human Binding pKi = 7.1 7.1 -5 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
71455896 83805 None 0 Human Binding pKi = 5.1 5.1 -3 5
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 266 2 1 3 1.3 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccn1 10.1016/j.bmcl.2012.08.046
CHEMBL2205832 83805 None 0 Human Binding pKi = 5.1 5.1 -3 5
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 266 2 1 3 1.3 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccn1 10.1016/j.bmcl.2012.08.046
10035281 100982 None 0 Human Binding pKi = 5.1 5.1 -1 8
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL294273 100982 None 0 Human Binding pKi = 5.1 5.1 -1 8
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
10035281 100982 None 0 Rat Binding pKi = 5.1 5.1 -3 8
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
CHEMBL294273 100982 None 0 Rat Binding pKi = 5.1 5.1 -3 8
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
10035281 100982 None 0 Human Binding pKi = 5.1 5.1 -1 8
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
CHEMBL294273 100982 None 0 Human Binding pKi = 5.1 5.1 -1 8
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
10871551 120511 None 0 Human Binding pKi = 6.1 6.1 -7 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120511 None 0 Human Binding pKi = 6.1 6.1 -7 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
11000399 59095 None 0 Human Binding pKi = 5.1 5.1 -1 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 59095 None 0 Human Binding pKi = 5.1 5.1 -1 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
44318766 205751 None 0 Human Binding pKi = 6.1 6.1 3 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
CHEMBL82754 205751 None 0 Human Binding pKi = 6.1 6.1 3 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
44318851 104726 None 0 Human Binding pKi = 7.1 7.1 -1 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL310558 104726 None 0 Human Binding pKi = 7.1 7.1 -1 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
11131099 120261 None 0 Human Binding pKi = 5.1 5.1 -8 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 120261 None 0 Human Binding pKi = 5.1 5.1 -8 5
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
187 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
187.0 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
294 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
65 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
145961152 161591 None 0 Human Binding pKi = 5.1 5.1 -5 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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 161591 None 0 Human Binding pKi = 5.1 5.1 -5 5
Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M4 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
68764898 672 None 2 Human Binding pKi = 6.1 6.1 -2 3
Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 672 None 2 Human Binding pKi = 6.1 6.1 -2 3
Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 672 None 2 Human Binding pKi = 6.1 6.1 -2 3
Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
162353383 182577 None 0 Human Binding pKi = 5.1 5.1 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 182577 None 0 Human Binding pKi = 5.1 5.1 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
11110049 58240 None 0 Human Binding pKi = 4.1 4.1 -2 4
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2ccncc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL168223 58240 None 0 Human Binding pKi = 4.1 4.1 -2 4
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2ccncc2)c2ccccc2C1 10.1021/jm020895l
162353387 181231 None 0 Human Binding pKi = 4.1 4.1 -2 2
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 2 1 3 2.2 O=C(CN1CCCc2ccc(O)cc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4761549 181231 None 0 Human Binding pKi = 4.1 4.1 -2 2
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 2 1 3 2.2 O=C(CN1CCCc2ccc(O)cc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
44422692 11853 None 0 Human Binding pKi = 4.1 4.1 -9 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 11853 None 0 Human Binding pKi = 4.1 4.1 -9 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 11853 None 0 Human Binding pKi = 4.1 4.1 -9 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
3675988 176835 None 66 Human Binding pKi = 4.1 4.1 -7 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc(C2CCCN2)c1 10.1021/jm800145d
CHEMBL461087 176835 None 66 Human Binding pKi = 4.1 4.1 -7 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc(C2CCCN2)c1 10.1021/jm800145d
44446841 12338 None 0 Human Binding pKi = 4.1 4.1 -5 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 12338 None 0 Human Binding pKi = 4.1 4.1 -5 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 12338 None 0 Human Binding pKi = 4.1 4.1 -5 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
46227481 14139 None 0 Human Binding pKi = 4.1 4.1 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14139 None 0 Human Binding pKi = 4.1 4.1 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14139 None 0 Human Binding pKi = 4.1 4.1 -1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
155523889 176524 None 0 Human Binding pKi = 7.1 7.1 -11 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176524 None 0 Human Binding pKi = 7.1 7.1 -11 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176524 None 0 Human Binding pKi = 7.1 7.1 -11 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
73345823 89815 None 0 Human Binding pKi = 7.1 7.1 -14 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 89815 None 0 Human Binding pKi = 7.1 7.1 -14 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
4212 198679 None 82 Human Binding pKi = 7.1 7.1 -1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
CHEMBL1417019 198679 None 82 Human Binding pKi = 7.1 7.1 -1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
CHEMBL58 198679 None 82 Human Binding pKi = 7.1 7.1 -1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 nan
10315426 101048 None 0 Human Binding pKi = 6.1 6.1 -2 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 101048 None 0 Human Binding pKi = 6.1 6.1 -2 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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
44299616 195708 None 0 Human Binding pKi = 6.1 6.1 1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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 195708 None 0 Human Binding pKi = 6.1 6.1 1 4
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) 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
133640439 181373 None 1 Human Binding pKi = 6.1 6.1 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181373 None 1 Human Binding pKi = 6.1 6.1 -1 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
162353377 181165 None 0 Human Binding pKi = 5.1 5.1 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 181165 None 0 Human Binding pKi = 5.1 5.1 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
657347 5076 None 2 Human Binding pKi = 5.1 5.1 -75 6
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 5076 None 2 Human Binding pKi = 5.1 5.1 -75 6
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 5076 None 2 Human Binding pKi = 5.1 5.1 -75 6
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
44274477 165568 None 0 Human Binding pKi = 4.1 4.1 -3 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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 165568 None 0 Human Binding pKi = 4.1 4.1 -3 5
Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.Affinity for Muscarinic acetylcholine receptor M4 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
7047822 176836 None 15 Human Binding pKi = 4.1 4.1 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 176836 None 15 Human Binding pKi = 4.1 4.1 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@H]2CCCN2)c1 10.1021/jm800145d
73346334 92541 None 0 Human Binding pKi = 6.1 6.1 1 7
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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 92541 None 0 Human Binding pKi = 6.1 6.1 1 7
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 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
10225340 204334 None 0 Human Binding pKi = 8.0 8.0 -2 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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 204334 None 0 Human Binding pKi = 8.0 8.0 -2 4
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
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
410345 89803 None 4 Human Binding pKi = 8.0 8.0 -1 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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 89803 None 4 Human Binding pKi = 8.0 8.0 -1 4
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M4 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
156014820 178305 None 0 Human Binding pKi = 8.0 8.0 -4 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178305 None 0 Human Binding pKi = 8.0 8.0 -4 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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 178305 None 0 Human Binding pKi = 8.0 8.0 -4 5
Displacement of [3H]-NMS from human muscarinic M4 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M4 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
156014820 178305 None 0 Human Binding pKi = 8.0 8.0 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178305 None 0 Human Binding pKi = 8.0 8.0 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 178305 None 0 Human Binding pKi = 8.0 8.0 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
10035281 100982 None 0 Human Binding pKi = 6.1 6.1 -1 8
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL294273 100982 None 0 Human Binding pKi = 6.1 6.1 -1 8
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
9937474 170470 None 0 Human Binding pKi = 7.0 7.0 -457 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 170470 None 0 Human Binding pKi = 7.0 7.0 -457 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
10421982 206041 None 0 Human Binding pKi = 6.0 6.0 -1 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
CHEMBL85190 206041 None 0 Human Binding pKi = 6.0 6.0 -1 4
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranesInhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
3055 1433 None 44 Human Binding pKi = 6.0 6.0 -1 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 1433 None 44 Human Binding pKi = 6.0 6.0 -1 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 1433 None 44 Human Binding pKi = 6.0 6.0 -1 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 1433 None 44 Human Binding pKi = 6.0 6.0 -1 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 1433 None 44 Human Binding pKi = 6.0 6.0 -1 9
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
171578 12304 None 5 Human Binding pKi = 5.0 5.0 -4 5
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 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 12304 None 5 Human Binding pKi = 5.0 5.0 -4 5
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 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 12304 None 5 Human Binding pKi = 5.0 5.0 -4 5
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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 2473 None 6 Human Binding pKi = 5.0 5.0 -4 7
Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M4 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
162657652 180985 None 0 Human Binding pKi = 4.0 4.0 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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 180985 None 0 Human Binding pKi = 4.0 4.0 -2 4
Displacement of [3H]-NMS from muscarinic M4 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M4 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
16086061 80218 None 0 Human Binding pKi = 7.0 7.0 -99 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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 80218 None 0 Human Binding pKi = 7.0 7.0 -99 5
Inhibition of [3H]NMS binding to human cloned M4 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M4 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
155554262 176555 None 0 Human Binding pKi = 7.0 7.0 -2 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176555 None 0 Human Binding pKi = 7.0 7.0 -2 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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 176555 None 0 Human Binding pKi = 7.0 7.0 -2 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M4 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
44593620 187936 None 0 Human Binding pKi = 7.0 7.0 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 187936 None 0 Human Binding pKi = 7.0 7.0 -3 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
164614994 188502 None 0 Human Binding pKi = 6.0 6.0 -77 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188502 None 0 Human Binding pKi = 6.0 6.0 -77 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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 188502 None 0 Human Binding pKi = 6.0 6.0 -77 5
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 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
164627387 188606 None 0 Human Binding pKi = 5.0 5.0 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4874785 188606 None 0 Human Binding pKi = 5.0 5.0 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028995 188606 None 0 Human Binding pKi = 5.0 5.0 -7 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 832 19 12 11 -1.4 CC(=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCC(=O)NC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
137640511 157066 None 0 Human Binding pKi = 5.0 5.0 -36 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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 157066 None 0 Human Binding pKi = 5.0 5.0 -36 8
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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
14925759 158038 None 6 Human Binding pKi = 5.0 5.0 -3235 13
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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 158038 None 6 Human Binding pKi = 5.0 5.0 -3235 13
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M4 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
46227555 14131 None 1 Human Binding pKi = 4.0 4.0 -8 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14131 None 1 Human Binding pKi = 4.0 4.0 -8 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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 14131 None 1 Human Binding pKi = 4.0 4.0 -8 4
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M4 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
44439392 91782 None 0 Human Binding pKi = 4.0 4.0 -4677 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 336 5 2 2 5.1 CCCSc1ccccc1CC1NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2007.01.093
CHEMBL241100 91782 None 0 Human Binding pKi = 4.0 4.0 -4677 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 336 5 2 2 5.1 CCCSc1ccccc1CC1NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2007.01.093
118719930 115784 None 0 Human Binding pKi = 7.0 7.0 1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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 115784 None 0 Human Binding pKi = 7.0 7.0 1 5
Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M4 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
44576913 193314 None 0 Human Binding pKi = 7.0 7.0 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 193314 None 0 Human Binding pKi = 7.0 7.0 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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 193314 None 0 Human Binding pKi = 7.0 7.0 -4 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M4 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
44439393 91809 None 0 Human Binding pKi = 4.0 4.0 -2754 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 308 3 2 2 4.3 CSc1ccccc1CC1NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2007.01.093
CHEMBL241279 91809 None 0 Human Binding pKi = 4.0 4.0 -2754 2
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
ChEMBL 308 3 2 2 4.3 CSc1ccccc1CC1NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2007.01.093
164624458 188583 None 0 Human Binding pKi = 5.0 5.0 -29 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 873 19 9 12 -0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4863121 188583 None 0 Human Binding pKi = 5.0 5.0 -29 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 873 19 9 12 -0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028823 188583 None 0 Human Binding pKi = 5.0 5.0 -29 3
Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M4 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 873 19 9 12 -0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(C(=O)CC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44318817 169114 None 0 Human Binding pKi = 6.0 6.0 -5 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL440138 169114 None 0 Human Binding pKi = 6.0 6.0 -5 4
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
11808040 168395 None 0 Human Binding pKi = 7.0 7.0 -7 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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 168395 None 0 Human Binding pKi = 7.0 7.0 -7 6
Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M4 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
156017826 177858 None 0 Human Binding pKi = 7.0 7.0 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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 177858 None 0 Human Binding pKi = 7.0 7.0 -4 5
Displacement of [3H]NMS from human recombinant muscarinic receptor M4 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M4 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
10951142 5222 None 0 Human Binding pKi = 7.0 7.0 -1 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5222 None 0 Human Binding pKi = 7.0 7.0 -1 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
71459604 83793 None 0 Human Binding pKi = 6.0 6.0 -1 14
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83793 None 0 Human Binding pKi = 6.0 6.0 -1 14
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
2229 464 None 22 Human Binding pKi = 6.0 6.0 -2 6
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
295 464 None 22 Human Binding pKi = 6.0 6.0 -2 6
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
CHEMBL128365 464 None 22 Human Binding pKi = 6.0 6.0 -2 6
Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M4 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
44448575 11917 None 0 Human Binding pKi = 5.0 5.0 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11917 None 0 Human Binding pKi = 5.0 5.0 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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 11917 None 0 Human Binding pKi = 5.0 5.0 -1 5
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M4 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
24865895 96005 None 0 Human Binding pKi = 5.0 5.0 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 96005 None 0 Human Binding pKi = 5.0 5.0 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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 96005 None 0 Human Binding pKi = 5.0 5.0 -3 5
Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M4 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
11729182 5231 None 0 Human Binding pKi = 5.0 5.0 -2 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 5231 None 0 Human Binding pKi = 5.0 5.0 -2 5
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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
2745 3861 None 42 Human Binding pIC50 = 8.1 8.1 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3861 None 42 Human Binding pIC50 = 8.1 8.1 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
5572.0 3861 None 42 Human Binding pIC50 = 8.1 8.1 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3861 None 42 Human Binding pIC50 = 8.1 8.1 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3861 None 42 Human Binding pIC50 = 8.1 8.1 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3861 None 42 Human Binding pIC50 = 8.1 8.1 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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 3861 None 42 Human Binding pIC50 = 8.1 8.1 -5 8
Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m4 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
11434515 261 None 6 Human Binding pIC50 = 8.0 8.0 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
11434515.0 261 None 6 Human Binding pIC50 = 8.0 8.0 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
11519741 261 None 6 Human Binding pIC50 = 8.0 8.0 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
4484 261 None 6 Human Binding pIC50 = 8.0 8.0 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
7449 261 None 6 Human Binding pIC50 = 8.0 8.0 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
CHEMBL1194325 261 None 6 Human Binding pIC50 = 8.0 8.0 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
DB08897 261 None 6 Human Binding pIC50 = 8.0 8.0 1 5
Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
15376 3994 None 0 Human Binding pKd = 8.4 8.4 -4 4
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
349 3994 None 0 Human Binding pKd = 8.4 8.4 -4 4
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
3643 3994 None 0 Human Binding pKd = 8.4 8.4 -4 4
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
CHEMBL1165342 3994 None 0 Human Binding pKd = 8.4 8.4 -4 4
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
DB13374 3994 None 0 Human Binding pKd = 8.4 8.4 -4 4
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
2824 3993 None 0 Human Binding pKd = 8.3 8.3 -1 4
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
345 3993 None 0 Human Binding pKd = 8.3 8.3 -1 4
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
71203 3993 None 0 Human Binding pKd = 8.3 8.3 -1 4
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
CHEMBL1892145 3993 None 0 Human Binding pKd = 8.3 8.3 -1 4
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
DB13793 3993 None 0 Human Binding pKd = 8.3 8.3 -1 4
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
92112 21705 None 18 Human Binding pKd = 8.3 8.3 -1 4
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@@]12CCCN3CCc4c(n(c5ccccc45)C(=O)C1)[C@H]32 None
CHEMBL1318553 21705 None 18 Human Binding pKd = 8.3 8.3 -1 4
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@@]12CCCN3CCc4c(n(c5ccccc45)C(=O)C1)[C@H]32 None
2360 3693 None 43 Human Binding pKd = 8.3 8.3 -1 5
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 3693 None 43 Human Binding pKd = 8.3 8.3 -1 5
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 3693 None 43 Human Binding pKd = 8.3 8.3 -1 5
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 3693 None 43 Human Binding pKd = 8.3 8.3 -1 5
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 3693 None 43 Human Binding pKd = 8.3 8.3 -1 5
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 3693 None 43 Human Binding pKd = 8.3 8.3 -1 5
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
2381 663 None 48 Human Binding pKd = 8.1 8.1 -9 8
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
2381.0 663 None 48 Human Binding pKd = 8.1 8.1 -9 8
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
374 663 None 48 Human Binding pKd = 8.1 8.1 -9 8
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
7128 663 None 48 Human Binding pKd = 8.1 8.1 -9 8
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
CHEMBL1101 663 None 48 Human Binding pKd = 8.1 8.1 -9 8
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
DB00810 663 None 48 Human Binding pKd = 8.1 8.1 -9 8
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
23724781.0 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
23724781.0 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
23724781.0 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
23724781.0 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
23724781.0 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
23724781.0 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
316 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
CHEMBL1354199 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
CHEMBL1354199 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
CHEMBL1354199 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
CHEMBL1354199 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
CHEMBL1354199 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
CHEMBL1354199 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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 2835 None 19 Human Binding pKd = 10.0 10.0 -9 9
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
23056 112 None 29 Human Binding pKd = 10.1 10.1 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 2841607
23056 112 None 29 Human Binding pKd = 10.1 10.1 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
318 112 None 29 Human Binding pKd = 10.1 10.1 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 2841607
318 112 None 29 Human Binding pKd = 10.1 10.1 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
3260 112 None 29 Human Binding pKd = 10.1 10.1 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 2841607
3260 112 None 29 Human Binding pKd = 10.1 10.1 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
CHEMBL12980 112 None 29 Human Binding pKd = 10.1 10.1 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 2841607
CHEMBL12980 112 None 29 Human Binding pKd = 10.1 10.1 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
348 3803 None 0 Human Binding pKd = 4 4.0 -2 4
UnclassifiedUnclassified
Guide to Pharmacology 262 2 1 6 1.9 OCCc1sc2=Nc3c(Cn2c1C)cnc(n3)C 14722259
66706 3803 None 0 Human Binding pKd = 4 4.0 -2 4
UnclassifiedUnclassified
Guide to Pharmacology 262 2 1 6 1.9 OCCc1sc2=Nc3c(Cn2c1C)cnc(n3)C 14722259
57664406 2398 None 50 Human Binding pKd = 5.5 5.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 24807965
6938 2398 None 50 Human Binding pKd = 5.5 5.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 24807965
CHEMBL4089376 2398 None 50 Human Binding pKd = 5.5 5.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology 437 5 2 7 1.9 CN1CCN(CC1)C(=O)COc1nc2sc(c(c2c(c1Cl)C)N)C(=O)NC1CC1 24807965
107867 2974 None 55 Human Binding pKd = 7 7.0 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 8759038
309 2974 None 55 Human Binding pKd = 7 7.0 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 8759038
CHEMBL17045 2974 None 55 Human Binding pKd = 7 7.0 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 8759038
187 255 None 39 Human Binding pKd = 8.2 8.2 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 14722259
187.0 255 None 39 Human Binding pKd = 8.2 8.2 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 14722259
294 255 None 39 Human Binding pKd = 8.2 8.2 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 14722259
65 255 None 39 Human Binding pKd = 8.2 8.2 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 14722259
8593 255 None 39 Human Binding pKd = 8.2 8.2 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 14722259
CHEMBL667 255 None 39 Human Binding pKd = 8.2 8.2 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 14722259
DB03128 255 None 39 Human Binding pKd = 8.2 8.2 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 14722259
2381 663 None 48 Human Binding pKd = 8.6 8.6 -9 8
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
2381.0 663 None 48 Human Binding pKd = 8.6 8.6 -9 8
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
374 663 None 48 Human Binding pKd = 8.6 8.6 -9 8
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
7128 663 None 48 Human Binding pKd = 8.6 8.6 -9 8
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
CHEMBL1101 663 None 48 Human Binding pKd = 8.6 8.6 -9 8
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
DB00810 663 None 48 Human Binding pKd = 8.6 8.6 -9 8
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
119357 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1941609
119357 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 29515448
119357 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 32079174
3264 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1941609
3264 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 29515448
3264 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 32079174
368 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1941609
368 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 29515448
368 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 32079174
CHEMBL279453 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1941609
CHEMBL279453 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 29515448
CHEMBL279453 304 None 49 Human Binding pKd = 8.7 8.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 32079174
21123938 733 None 0 Human Binding pKd None 3.6 3.6 1 5
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
343 733 None 0 Human Binding pKd None 3.6 3.6 1 5
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
15376 3994 None 0 Human Binding pKd None 4.2 4.2 -4 4
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 3994 None 0 Human Binding pKd None 4.2 4.2 -4 4
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 3994 None 0 Human Binding pKd None 4.2 4.2 -4 4
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 3994 None 0 Human Binding pKd None 4.2 4.2 -4 4
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 3994 None 0 Human Binding pKd None 4.2 4.2 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
344 2749 None 0 Human Binding pKd None 4.4 4.4 -1 5
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 2749 None 0 Human Binding pKd None 4.4 4.4 -1 5
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 2749 None 0 Human Binding pKd None 4.4 4.4 -1 5
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
332 2034 None 0 Human Binding pKd None 4.5 4.5 -1 5
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 2034 None 0 Human Binding pKd None 4.5 4.5 -1 5
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 2034 None 0 Human Binding pKd None 4.5 4.5 -1 5
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
2824 3993 None 0 Human Binding pKd None 4.6 4.6 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
345 3993 None 0 Human Binding pKd None 4.6 4.6 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
71203 3993 None 0 Human Binding pKd None 4.6 4.6 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
CHEMBL1892145 3993 None 0 Human Binding pKd None 4.6 4.6 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
DB13793 3993 None 0 Human Binding pKd None 4.6 4.6 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
2360 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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 3693 None 43 Human Binding pKd None 4.9 4.9 -1 5
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
346 3689 None 0 Human Binding pKd None 5.3 5.3 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 466 2 2 6 4.4 CN[C@@H]1C[C@H]2O[C@]([C@@H]1OC)(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
44259 3689 None 0 Human Binding pKd None 5.3 5.3 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 466 2 2 6 4.4 CN[C@@H]1C[C@H]2O[C@]([C@@H]1OC)(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
CHEMBL388978 3689 None 0 Human Binding pKd None 5.3 5.3 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 466 2 2 6 4.4 CN[C@@H]1C[C@H]2O[C@]([C@@H]1OC)(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
DB02010 3689 None 0 Human Binding pKd None 5.3 5.3 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 466 2 2 6 4.4 CN[C@@H]1C[C@H]2O[C@]([C@@H]1OC)(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
342 732 None 55 Human Binding pKd None 5.4 5.4 4 5
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
342 732 None 55 Human Binding pKd None 5.4 5.4 4 5
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 732 None 55 Human Binding pKd None 5.4 5.4 4 5
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 732 None 55 Human Binding pKd None 5.4 5.4 4 5
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 732 None 55 Human Binding pKd None 5.4 5.4 4 5
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 732 None 55 Human Binding pKd None 5.4 5.4 4 5
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
341 340 None 0 Human Binding pKd None 5.6 5.6 -7 4
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 340 None 0 Human Binding pKd None 5.6 5.6 -7 4
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
335 1836 None 0 Human Binding pKd None 5.7 5.7 -1 4
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 1836 None 0 Human Binding pKd None 5.7 5.7 -1 4
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 1836 None 0 Human Binding pKd None 5.7 5.7 -1 4
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
15118529 4083 None 0 Human Binding pKd None 5.9 5.9 2 4
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 4083 None 0 Human Binding pKd None 5.9 5.9 2 4
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 4083 None 0 Human Binding pKd None 5.9 5.9 2 4
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
339 4081 None 0 Human Binding pKd None 6.2 6.2 1 4
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 4081 None 0 Human Binding pKd None 6.2 6.2 1 4
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 4081 None 0 Human Binding pKd None 6.2 6.2 1 4
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
16219545 2200 None 0 Human Binding pKd None 6.4 6.4 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 537 6 2 7 5.6 CCCCCCOC(=O)[C@@]1(O)C[C@@H]2O[C@@]1(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
337 2200 None 0 Human Binding pKd None 6.4 6.4 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 537 6 2 7 5.6 CCCCCCOC(=O)[C@@]1(O)C[C@@H]2O[C@@]1(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3CNC1=O 10860942
42519285 2577 None 15 Human Binding pKi < 4.5 4.5 -60 5
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 2577 None 15 Human Binding pKi < 4.5 4.5 -60 5
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 2577 None 15 Human Binding pKi < 4.5 4.5 -60 5
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
23056 112 3H-QNB 29 Human Binding pKi = 10.5 10.5 -1 8
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
318 112 3H-QNB 29 Human Binding pKi = 10.5 10.5 -1 8
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
3260 112 3H-QNB 29 Human Binding pKi = 10.5 10.5 -1 8
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
CHEMBL12980 112 3H-QNB 29 Human Binding pKi = 10.5 10.5 -1 8
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
23056 112 3H-QNB 29 Human Binding pKi = 10.4 10.4 -1 8
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
318 112 3H-QNB 29 Human Binding pKi = 10.4 10.4 -1 8
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
3260 112 3H-QNB 29 Human Binding pKi = 10.4 10.4 -1 8
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
CHEMBL12980 112 3H-QNB 29 Human Binding pKi = 10.4 10.4 -1 8
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
12057539 208041 3H-QNB 42 Human Binding pKi = 10 10.0 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 3H-QNB 42 Human Binding pKi = 10 10.0 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 3H-QNB 42 Human Binding pKi = 10 10.0 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
325 2062 3H-NMS 0 Human Binding pKi = 9.9 9.9 -1 8
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
3746 2062 3H-NMS 0 Human Binding pKi = 9.9 9.9 -1 8
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
657308 2062 3H-NMS 0 Human Binding pKi = 9.9 9.9 -1 8
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
CHEMBL1615433 2062 3H-NMS 0 Human Binding pKi = 9.9 9.9 -1 8
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
DB00332 2062 3H-NMS 0 Human Binding pKi = 9.9 9.9 -1 8
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
131632304 216037 3H-QNB 0 Rat Binding pKi = 9.9 9.9 1 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
5184.0 216037 3H-QNB 0 Rat Binding pKi = 9.9 9.9 1 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
CHEMBL13030 216037 3H-QNB 0 Rat Binding pKi = 9.9 9.9 1 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
DB00747 216037 3H-QNB 0 Rat Binding pKi = 9.9 9.9 1 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
131632304 216037 3H-QNB 0 Human Binding pKi = 9.7 9.7 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
5184.0 216037 3H-QNB 0 Human Binding pKi = 9.7 9.7 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
CHEMBL13030 216037 3H-QNB 0 Human Binding pKi = 9.7 9.7 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
DB00747 216037 3H-QNB 0 Human Binding pKi = 9.7 9.7 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
131632304 216037 3H-NMS 0 Human Binding pKi = 9.7 9.7 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
5184.0 216037 3H-NMS 0 Human Binding pKi = 9.7 9.7 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
CHEMBL13030 216037 3H-NMS 0 Human Binding pKi = 9.7 9.7 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
DB00747 216037 3H-NMS 0 Human Binding pKi = 9.7 9.7 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
12057539 208041 3H-NMS 42 Human Binding pKi = 9.6 9.6 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 3H-NMS 42 Human Binding pKi = 9.6 9.6 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 3H-NMS 42 Human Binding pKi = 9.6 9.6 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
12057539 208041 3H-NMS 42 Human Binding pKi = 9.5 9.5 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
12057539 208041 3H-NMSP 42 Human Binding pKi = 9.5 9.5 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 3H-NMS 42 Human Binding pKi = 9.5 9.5 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 3H-NMSP 42 Human Binding pKi = 9.5 9.5 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 3H-NMS 42 Human Binding pKi = 9.5 9.5 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 3H-NMSP 42 Human Binding pKi = 9.5 9.5 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
12057539 208041 3H-NMS 42 Human Binding pKi = 9.5 9.5 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 3H-NMS 42 Human Binding pKi = 9.5 9.5 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 3H-NMS 42 Human Binding pKi = 9.5 9.5 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
132947 3864 3H-QNB 9 Rat Binding pKi = 9.4 9.4 -15 9
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 3864 3H-QNB 9 Rat Binding pKi = 9.4 9.4 -15 9
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 3864 3H-QNB 9 Rat Binding pKi = 9.4 9.4 -15 9
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
2028 2979 3H-NMS 80 Human Binding pKi = 9.4 9.4 -1 10
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2979 3H-NMS 80 Human Binding pKi = 9.4 9.4 -1 10
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2979 3H-NMS 80 Human Binding pKi = 9.4 9.4 -1 10
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634.0 2979 3H-NMS 80 Human Binding pKi = 9.4 9.4 -1 10
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2979 3H-NMS 80 Human Binding pKi = 9.4 9.4 -1 10
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2979 3H-NMS 80 Human Binding pKi = 9.4 9.4 -1 10
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
42470 216183 3H-NMS 0 Human Binding pKi = 9.3 9.3 2 5
NoneNone
PDSP KiDatabase 345 10 0 3 4.9 CCN(CCCC(=O)C1CCCCC1)C(C)CC2=CC=C(C=C2)OC None
42470 216183 3H-NMS 0 Human Binding pKi = 9.3 9.3 2 5
NoneNone
PDSP KiDatabase 345 10 0 3 4.9 CCN(CCCC(=O)C1CCCCC1)C(C)CC2=CC=C(C=C2)OC None
1734 116 3H-QNB 10 Human Binding pKi = 9.2 9.2 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-QNB 10 Human Binding pKi = 9.2 9.2 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-QNB 10 Human Binding pKi = 9.2 9.2 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
12057539 208041 3H-QNB 42 Human Binding pKi = 9.2 9.2 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 3H-QNB 42 Human Binding pKi = 9.2 9.2 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 3H-QNB 42 Human Binding pKi = 9.2 9.2 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
325 2062 3H-NMS 0 Human Binding pKi = 9.2 9.2 -1 8
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
3746 2062 3H-NMS 0 Human Binding pKi = 9.2 9.2 -1 8
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
657308 2062 3H-NMS 0 Human Binding pKi = 9.2 9.2 -1 8
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
CHEMBL1615433 2062 3H-NMS 0 Human Binding pKi = 9.2 9.2 -1 8
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
DB00332 2062 3H-NMS 0 Human Binding pKi = 9.2 9.2 -1 8
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
131632304 216037 3H-QNB 0 Human Binding pKi = 9.1 9.1 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
5184.0 216037 3H-QNB 0 Human Binding pKi = 9.1 9.1 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
CHEMBL13030 216037 3H-QNB 0 Human Binding pKi = 9.1 9.1 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
DB00747 216037 3H-QNB 0 Human Binding pKi = 9.1 9.1 -2 12
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
2745 3861 3H-NMS 42 Human Binding pKi = 9.1 9.1 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3861 3H-NMS 42 Human Binding pKi = 9.1 9.1 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572.0 3861 3H-NMS 42 Human Binding pKi = 9.1 9.1 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3861 3H-NMS 42 Human Binding pKi = 9.1 9.1 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3861 3H-NMS 42 Human Binding pKi = 9.1 9.1 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3861 3H-NMS 42 Human Binding pKi = 9.1 9.1 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3861 3H-NMS 42 Human Binding pKi = 9.1 9.1 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
3246155 215962 3H-NMS 0 Human Binding pKi = 9.1 9.1 -4 16
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
132947 3864 3H-QNB 9 Human Binding pKi = 9.0 9.0 -22 9
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 3864 3H-QNB 9 Human Binding pKi = 9.0 9.0 -22 9
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 3864 3H-QNB 9 Human Binding pKi = 9.0 9.0 -22 9
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
12057539 208041 3H-Arachidonic Acid 42 Human Binding pKi = 9 9.0 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 3H-Arachidonic Acid 42 Human Binding pKi = 9 9.0 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 3H-Arachidonic Acid 42 Human Binding pKi = 9 9.0 -1 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
154734599 2503 3H-QNB 12 Rat Binding pKi = 9.0 9.0 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-QNB 12 Rat Binding pKi = 9.0 9.0 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-QNB 12 Rat Binding pKi = 9.0 9.0 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-QNB 12 Rat Binding pKi = 9.0 9.0 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
12057539 208041 3H-cAMP 42 Rat Binding pKi = 9.0 9.0 -5 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 3H-cAMP 42 Rat Binding pKi = 9.0 9.0 -5 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 3H-cAMP 42 Rat Binding pKi = 9.0 9.0 -5 20
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3246155 215962 3H-QNB 0 Human Binding pKi = 9.0 9.0 -4 16
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
1734 116 3H-NMS 10 Human Binding pKi = 8.9 8.9 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-NMS 10 Human Binding pKi = 8.9 8.9 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-NMS 10 Human Binding pKi = 8.9 8.9 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
1734 116 3H-4-DAMP 10 Human Binding pKi = 8.9 8.9 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-4-DAMP 10 Human Binding pKi = 8.9 8.9 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-4-DAMP 10 Human Binding pKi = 8.9 8.9 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
1734 116 3H-cAMP 10 Rat Binding pKi = 8.9 8.9 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-cAMP 10 Rat Binding pKi = 8.9 8.9 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-cAMP 10 Rat Binding pKi = 8.9 8.9 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
1734 116 3H-NMS 10 Human Binding pKi = 8.9 8.9 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-NMS 10 Human Binding pKi = 8.9 8.9 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-NMS 10 Human Binding pKi = 8.9 8.9 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
3042 1414 3H-NMS 35 Human Binding pKi = 8.8 8.8 -1 14
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
3042.0 1414 3H-NMS 35 Human Binding pKi = 8.8 8.8 -1 14
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1414 3H-NMS 35 Human Binding pKi = 8.8 8.8 -1 14
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1414 3H-NMS 35 Human Binding pKi = 8.8 8.8 -1 14
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1414 3H-NMS 35 Human Binding pKi = 8.8 8.8 -1 14
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1414 3H-NMS 35 Human Binding pKi = 8.8 8.8 -1 14
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
1734 116 3H-QNB 10 Human Binding pKi = 8.8 8.8 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-QNB 10 Human Binding pKi = 8.8 8.8 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-QNB 10 Human Binding pKi = 8.8 8.8 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
2745 3861 3H-NMS 42 Human Binding pKi = 8.7 8.7 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3861 3H-NMS 42 Human Binding pKi = 8.7 8.7 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572.0 3861 3H-NMS 42 Human Binding pKi = 8.7 8.7 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3861 3H-NMS 42 Human Binding pKi = 8.7 8.7 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3861 3H-NMS 42 Human Binding pKi = 8.7 8.7 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3861 3H-NMS 42 Human Binding pKi = 8.7 8.7 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3861 3H-NMS 42 Human Binding pKi = 8.7 8.7 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
135398745 2914 3H-NMS 112 Human Binding pKi = 8 8.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2914 3H-QNB 112 Human Binding pKi = 8 8.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-NMS 112 Human Binding pKi = 8 8.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-QNB 112 Human Binding pKi = 8 8.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-NMS 112 Human Binding pKi = 8 8.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-QNB 112 Human Binding pKi = 8 8.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-NMS 112 Human Binding pKi = 8 8.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-QNB 112 Human Binding pKi = 8 8.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-NMS 112 Human Binding pKi = 8 8.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-QNB 112 Human Binding pKi = 8 8.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
154825138 216038 3H-4-DAMP 0 Human Binding pKi = 8 8.0 1 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
None 216258 3H-NMS 0 Human Binding pKi = 8 8.0 -1 5
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
23724781.0 2835 None 19 Human Binding pKi = 8 8.0 -9 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
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
316 2835 None 19 Human Binding pKi = 8 8.0 -9 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
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 2835 None 19 Human Binding pKi = 8 8.0 -9 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
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 2835 None 19 Human Binding pKi = 8 8.0 -9 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
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
CHEMBL1354199 2835 None 19 Human Binding pKi = 8 8.0 -9 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
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 2835 None 19 Human Binding pKi = 8 8.0 -9 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
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 2835 None 19 Human Binding pKi = 8 8.0 -9 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
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 2835 None 19 Human Binding pKi = 8 8.0 -9 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
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
2293 3186 None 27 Human Binding pKi = 8.0 8.0 1 4
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
329 3186 None 27 Human Binding pKi = 8.0 8.0 1 4
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
4934 3186 None 27 Human Binding pKi = 8.0 8.0 1 4
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
4934.0 3186 None 27 Human Binding pKi = 8.0 8.0 1 4
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
CHEMBL1180725 3186 None 27 Human Binding pKi = 8.0 8.0 1 4
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
DB00782 3186 None 27 Human Binding pKi = 8.0 8.0 1 4
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
11519069 3939 None 3 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
11519070 3939 None 3 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
11519070.0 3939 None 3 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
4816 3939 None 3 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
7354 3939 None 3 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
CHEMBL1187833 3939 None 3 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
DB09076 3939 None 3 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
154825138 216038 3H-QNB 0 Human Binding pKi = 8.0 8.0 1 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
310 1922 3H-NMS 0 Human Binding pKi = 8.0 8.0 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
3602 1922 3H-NMS 0 Human Binding pKi = 8.0 8.0 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
CHEMBL3545990 1922 3H-NMS 0 Human Binding pKi = 8.0 8.0 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
154825138 216038 3H-NMS 0 Human Binding pKi = 8.0 8.0 1 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
308 2060 3H-NMS 23 Mouse Binding pKi = 7 7.0 -4 9
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
3603 2060 3H-NMS 23 Mouse Binding pKi = 7 7.0 -4 9
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
CHEMBL1256682 2060 3H-NMS 23 Mouse Binding pKi = 7 7.0 -4 9
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
154734599 2503 3H-NMS 12 Rat Binding pKi = 7 7.0 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-NMS 12 Rat Binding pKi = 7 7.0 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-NMS 12 Rat Binding pKi = 7 7.0 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-NMS 12 Rat Binding pKi = 7 7.0 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
10090005 215986 3H-QNB 0 Human Binding pKi = 6 6.0 -1258 11
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
3075702 217332 3H-4-DAMP 0 Human Binding pKi = 6 6.0 -2 37
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
145 140 3H-QNB 49 Human Binding pKi = 5 5.0 -1949 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 3H-QNB 49 Human Binding pKi = 5 5.0 -1949 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 3H-QNB 49 Human Binding pKi = 5 5.0 -1949 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 3H-QNB 49 Human Binding pKi = 5 5.0 -1949 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
179 400 3H-QNB 115 Human Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 3H-QNB 115 Human Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159.0 400 3H-QNB 115 Human Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 3H-QNB 115 Human Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 3H-QNB 115 Human Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 3H-QNB 115 Human Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
141 1427 3H-QNB 35 Human Binding pKi = 5 5.0 -114 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1427 3H-QNB 35 Human Binding pKi = 5 5.0 -114 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1427 3H-QNB 35 Human Binding pKi = 5 5.0 -114 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1427 3H-QNB 35 Human Binding pKi = 5 5.0 -114 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
1353 1911 3H-QNB 93 Human Binding pKi = 5 5.0 -6918 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 3H-QNB 93 Human Binding pKi = 5 5.0 -6918 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559.0 1911 3H-QNB 93 Human Binding pKi = 5 5.0 -6918 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 3H-QNB 93 Human Binding pKi = 5 5.0 -6918 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 3H-QNB 93 Human Binding pKi = 5 5.0 -6918 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 3H-QNB 93 Human Binding pKi = 5 5.0 -6918 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1588 2325 3H-QNB 27 Human Binding pKi = 5 5.0 -28840 44
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 2325 3H-QNB 27 Human Binding pKi = 5 5.0 -28840 44
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
28864.0 2325 3H-QNB 27 Human Binding pKi = 5 5.0 -28840 44
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 2325 3H-QNB 27 Human Binding pKi = 5 5.0 -28840 44
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 2325 3H-QNB 27 Human Binding pKi = 5 5.0 -28840 44
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 2325 3H-QNB 27 Human Binding pKi = 5 5.0 -28840 44
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
134 2514 3H-QNB 24 Human Binding pKi = 5 5.0 -8511 67
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 2514 3H-QNB 24 Human Binding pKi = 5 5.0 -8511 67
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 2514 3H-QNB 24 Human Binding pKi = 5 5.0 -8511 67
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
9681.0 2514 3H-QNB 24 Human Binding pKi = 5 5.0 -8511 67
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 2514 3H-QNB 24 Human Binding pKi = 5 5.0 -8511 67
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 2514 3H-QNB 24 Human Binding pKi = 5 5.0 -8511 67
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
15897 2862 3H-QNB 0 Human Binding pKi = 5 5.0 -173 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2862 3H-QNB 0 Human Binding pKi = 5 5.0 -173 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2862 3H-QNB 0 Human Binding pKi = 5 5.0 -173 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
119570 3159 3H-QNB 96 Human Binding pKi = 5 5.0 -7585 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
119570.0 3159 3H-QNB 96 Human Binding pKi = 5 5.0 -7585 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 3H-QNB 96 Human Binding pKi = 5 5.0 -7585 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 3H-QNB 96 Human Binding pKi = 5 5.0 -7585 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 3H-QNB 96 Human Binding pKi = 5 5.0 -7585 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 3H-QNB 96 Human Binding pKi = 5 5.0 -7585 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2389 3331 3H-QNB 118 Human Binding pKi = 5 5.0 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 3H-QNB 118 Human Binding pKi = 5 5.0 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 3H-QNB 118 Human Binding pKi = 5 5.0 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 3H-QNB 118 Human Binding pKi = 5 5.0 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 3H-QNB 118 Human Binding pKi = 5 5.0 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 3H-QNB 118 Human Binding pKi = 5 5.0 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
128563 3464 3H-QNB 33 Human Binding pKi = 5 5.0 -2398 42
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 3464 3H-QNB 33 Human Binding pKi = 5 5.0 -2398 42
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 3464 3H-QNB 33 Human Binding pKi = 5 5.0 -2398 42
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 3464 3H-QNB 33 Human Binding pKi = 5 5.0 -2398 42
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
213 3853 3H-QNB 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3853 3H-QNB 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3853 3H-QNB 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533.0 3853 3H-QNB 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3853 3H-QNB 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3853 3H-QNB 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
185 4006 3H-QNB 60 Human Binding pKi = 5 5.0 -30902 37
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 4006 3H-QNB 60 Human Binding pKi = 5 5.0 -30902 37
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 4006 3H-QNB 60 Human Binding pKi = 5 5.0 -30902 37
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 4006 3H-QNB 60 Human Binding pKi = 5 5.0 -30902 37
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2865 4143 3H-QNB 73 Human Binding pKi = 5 5.0 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 3H-QNB 73 Human Binding pKi = 5 5.0 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 3H-QNB 73 Human Binding pKi = 5 5.0 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854.0 4143 3H-QNB 73 Human Binding pKi = 5 5.0 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 3H-QNB 73 Human Binding pKi = 5 5.0 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 3H-QNB 73 Human Binding pKi = 5 5.0 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
103 4153 3H-QNB 61 Human Binding pKi = 5 5.0 -190 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 3H-QNB 61 Human Binding pKi = 5 5.0 -190 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 3H-QNB 61 Human Binding pKi = 5 5.0 -190 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 3H-QNB 61 Human Binding pKi = 5 5.0 -190 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 3H-QNB 61 Human Binding pKi = 5 5.0 -190 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
10297 27112 3H-QNB 30 Human Binding pKi = 5 5.0 -38 42
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 27112 3H-QNB 30 Human Binding pKi = 5 5.0 -38 42
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
115237 55585 3H-QNB 119 Human Binding pKi = 5 5.0 -42657 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
115237.0 55585 3H-QNB 119 Human Binding pKi = 5 5.0 -42657 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 3H-QNB 119 Human Binding pKi = 5 5.0 -42657 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 55585 3H-QNB 119 Human Binding pKi = 5 5.0 -42657 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1979 77326 3H-cAMP 70 Human Binding pKi = 5 5.0 -13 4
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 77326 3H-cAMP 70 Human Binding pKi = 5 5.0 -13 4
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
3663 99967 3H-QNB 83 Human Binding pKi = 5 5.0 -288 29
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 99967 3H-QNB 83 Human Binding pKi = 5 5.0 -288 29
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
3036780.0 107531 3H-QNB 20 Human Binding pKi = 5 5.0 -58884 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 107531 3H-QNB 20 Human Binding pKi = 5 5.0 -58884 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 3H-QNB 20 Human Binding pKi = 5 5.0 -58884 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970.0 107531 3H-QNB 20 Human Binding pKi = 5 5.0 -58884 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 3H-QNB 20 Human Binding pKi = 5 5.0 -58884 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 3H-QNB 20 Human Binding pKi = 5 5.0 -58884 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 107531 3H-QNB 20 Human Binding pKi = 5 5.0 -58884 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 107531 3H-QNB 20 Human Binding pKi = 5 5.0 -58884 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
37632 111592 3H-QNB 28 Human Binding pKi = 5 5.0 -1 8
NoneNone
PDSP KiDatabase 351 3 0 5 3.3 CN(C)Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
CHEMBL328250 111592 3H-QNB 28 Human Binding pKi = 5 5.0 -1 8
NoneNone
PDSP KiDatabase 351 3 0 5 3.3 CN(C)Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
446220 133521 3H-QNB 14 Human Binding pKi = 5 5.0 -1778 45
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 133521 3H-QNB 14 Human Binding pKi = 5 5.0 -1778 45
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
44208932 140707 UNDEFINED 7 Human Binding pKi = 5 5.0 -89125 36
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 140707 UNDEFINED 7 Human Binding pKi = 5 5.0 -89125 36
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
5280343 188275 3H-QNB 124 Human Binding pKi = 5 5.0 -147 32
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 188275 3H-QNB 124 Human Binding pKi = 5 5.0 -147 32
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 188275 3H-QNB 124 Human Binding pKi = 5 5.0 -147 32
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 202274 3H-QNB 22 Human Binding pKi = 5 5.0 -239 43
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202274 3H-QNB 22 Human Binding pKi = 5 5.0 -239 43
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202274 3H-QNB 22 Human Binding pKi = 5 5.0 -239 43
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 203025 3H-QNB 92 Human Binding pKi = 5 5.0 -275 33
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 203025 3H-QNB 92 Human Binding pKi = 5 5.0 -275 33
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 203066 3H-QNB 87 Human Binding pKi = 5 5.0 -79 40
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 203066 3H-QNB 87 Human Binding pKi = 5 5.0 -79 40
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
1973 203483 3H-4-DAMP 15 Rat Binding pKi = 5 5.0 -3 36
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 203483 3H-4-DAMP 15 Rat Binding pKi = 5 5.0 -3 36
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 203483 3H-4-DAMP 15 Rat Binding pKi = 5 5.0 -3 36
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
202478 204687 3H-QNB 20 Human Binding pKi = 5 5.0 -97 25
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 204687 3H-QNB 20 Human Binding pKi = 5 5.0 -97 25
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
5311189 204841 3H-QNB 11 Human Binding pKi = 5 5.0 -194 27
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 204841 3H-QNB 11 Human Binding pKi = 5 5.0 -194 27
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 205341 3H-QNB 21 Human Binding pKi = 5 5.0 -141 21
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 205341 3H-QNB 21 Human Binding pKi = 5 5.0 -141 21
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 205341 3H-QNB 21 Human Binding pKi = 5 5.0 -141 21
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 205501 3H-QNB 72 Human Binding pKi = 5 5.0 -1 36
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 205501 3H-QNB 72 Human Binding pKi = 5 5.0 -1 36
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 205501 3H-QNB 72 Human Binding pKi = 5 5.0 -1 36
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
3337 206367 3H-QNB 27 Human Binding pKi = 5 5.0 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337.0 206367 3H-QNB 27 Human Binding pKi = 5 5.0 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 3H-QNB 27 Human Binding pKi = 5 5.0 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 3H-QNB 27 Human Binding pKi = 5 5.0 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 3H-QNB 27 Human Binding pKi = 5 5.0 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 3H-QNB 27 Human Binding pKi = 5 5.0 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206367 3H-QNB 27 Human Binding pKi = 5 5.0 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
444 206666 3H-QNB 53 Human Binding pKi = 5 5.0 -2089 18
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 None
CHEMBL894 206666 3H-QNB 53 Human Binding pKi = 5 5.0 -2089 18
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 None
11954224 215953 3H-QNB 0 Human Binding pKi = 5 5.0 -141253 58
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
3251.0 215953 3H-QNB 0 Human Binding pKi = 5 5.0 -141253 58
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
CHEMBL1982133 215953 3H-QNB 0 Human Binding pKi = 5 5.0 -141253 58
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
DB00696 215953 3H-QNB 0 Human Binding pKi = 5 5.0 -141253 58
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
11954259 215979 3H-QNB 0 Human Binding pKi = 5 5.0 -13182 43
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
11957621 216039 3H-QNB 0 Human Binding pKi = 5 5.0 -1 10
NoneNone
PDSP KiDatabase 203 3 2 3 1.3 COC1=C(C=CC(=C1)CCN)O.Cl None
11957621 216039 3H-QNB 0 Rat Binding pKi = 5 5.0 -1 10
NoneNone
PDSP KiDatabase 203 3 2 3 1.3 COC1=C(C=CC(=C1)CCN)O.Cl None
40589 216144 3H-QNB 0 Human Binding pKi = 5 5.0 -407 8
NoneNone
PDSP KiDatabase 377 7 0 6 2.5 CCC1=NN(C(=O)N1CC)CCCN2CCN(CC2)C3=CC(=CC=C3)Cl None
25137849 216179 3H-QNB 0 Human Binding pKi = 5 5.0 -4 40
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 216179 3H-QNB 0 Human Binding pKi = 5 5.0 -4 40
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 216239 3H-QNB 0 Human Binding pKi = 5 5.0 -70794 30
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 216307 3H-NMS 0 Human Binding pKi = 5 5.0 -1 5
NoneNone
PDSP KiDatabase 433 6 3 3 4.6 CC(CCC(=O)NCC(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C None
None 216311 3H-QNB 0 Human Binding pKi = 5 5.0 -1 33
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 216312 3H-QNB 0 Human Binding pKi = 5 5.0 -1 33
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 216313 3H-QNB 0 Human Binding pKi = 5 5.0 -1 33
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 216314 3H-QNB 0 Human Binding pKi = 5 5.0 -1 33
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 216315 3H-QNB 0 Human Binding pKi = 5 5.0 -1 28
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 216316 3H-QNB 0 Human Binding pKi = 5 5.0 -1 39
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 216317 3H-QNB 0 Human Binding pKi = 5 5.0 -1 38
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 216318 3H-QNB 0 Human Binding pKi = 5 5.0 -1 30
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 216325 3H-QNB 0 Human Binding pKi = 5 5.0 -13 40
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 216326 3H-QNB 0 Human Binding pKi = 5 5.0 -16 40
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 216327 3H-QNB 0 Human Binding pKi = 5 5.0 -16 28
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 216328 3H-QNB 0 Human Binding pKi = 5 5.0 -16 28
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 216329 3H-QNB 0 Human Binding pKi = 5 5.0 -3 28
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 216330 3H-QNB 0 Human Binding pKi = 5 5.0 -281 28
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 216331 3H-QNB 0 Human Binding pKi = 5 5.0 -1 28
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 216494 3H-NMS 0 Human Binding pKi = 5 5.0 -1 13
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
367 3824 None 12 Human Binding pKi = 8.0 8.0 -10 8
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 3824 None 12 Human Binding pKi = 8.0 8.0 -10 8
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
5487427.0 3824 None 12 Human Binding pKi = 8.0 8.0 -10 8
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 3824 None 12 Human Binding pKi = 8.0 8.0 -10 8
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 3824 None 12 Human Binding pKi = 8.0 8.0 -10 8
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 3824 None 12 Human Binding pKi = 8.0 8.0 -10 8
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 3824 None 12 Human Binding pKi = 8.0 8.0 -10 8
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 3824 None 12 Human Binding pKi = 8.0 8.0 -10 8
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
135398737 958 3H-QNB 93 Human Binding pKi = 8.0 8.0 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-QNB 93 Human Binding pKi = 8.0 8.0 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-QNB 93 Human Binding pKi = 8.0 8.0 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-QNB 93 Human Binding pKi = 8.0 8.0 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-QNB 93 Human Binding pKi = 8.0 8.0 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-QNB 93 Human Binding pKi = 8.0 8.0 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
4066 204626 3H-QNB 78 Human Binding pKi = 8.0 8.0 -1 7
NoneNone
PDSP KiDatabase 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
4066.0 204626 3H-QNB 78 Human Binding pKi = 8.0 8.0 -1 7
NoneNone
PDSP KiDatabase 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
CHEMBL73451 204626 3H-QNB 78 Human Binding pKi = 8.0 8.0 -1 7
NoneNone
PDSP KiDatabase 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
DB01071 204626 3H-QNB 78 Human Binding pKi = 8.0 8.0 -1 7
NoneNone
PDSP KiDatabase 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
308 2060 3H-NMS 23 Rat Binding pKi = 7.0 7.0 -4 9
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
3603 2060 3H-NMS 23 Rat Binding pKi = 7.0 7.0 -4 9
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
CHEMBL1256682 2060 3H-NMS 23 Rat Binding pKi = 7.0 7.0 -4 9
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
1224 1432 3H-QNB 83 Human Binding pKi = 7.0 7.0 -3 13
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 3H-QNB 83 Human Binding pKi = 7.0 7.0 -3 13
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100.0 1432 3H-QNB 83 Human Binding pKi = 7.0 7.0 -3 13
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 3H-QNB 83 Human Binding pKi = 7.0 7.0 -3 13
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 3H-QNB 83 Human Binding pKi = 7.0 7.0 -3 13
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 3H-QNB 83 Human Binding pKi = 7.0 7.0 -3 13
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 3H-QNB 83 Human Binding pKi = 7.0 7.0 -3 13
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1427 2013 3H-QNB 54 Human Binding pKi = 7.0 7.0 -2 27
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 3H-QNB 54 Human Binding pKi = 7.0 7.0 -2 27
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 3H-QNB 54 Human Binding pKi = 7.0 7.0 -2 27
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 3H-QNB 54 Human Binding pKi = 7.0 7.0 -2 27
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 3H-QNB 54 Human Binding pKi = 7.0 7.0 -2 27
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
62865 1274 3H-4-DAMP 0 Human Binding pKi = 7.9 7.9 -3 14
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 1274 3H-4-DAMP 0 Human Binding pKi = 7.9 7.9 -3 14
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 1274 3H-4-DAMP 0 Human Binding pKi = 7.9 7.9 -3 14
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 1274 3H-4-DAMP 0 Human Binding pKi = 7.9 7.9 -3 14
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 1274 3H-4-DAMP 0 Human Binding pKi = 7.9 7.9 -3 14
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
5387 94879 3H-QNB 31 Human Binding pKi = 7.9 7.9 -3 5
NoneNone
PDSP KiDatabase 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O None
CHEMBL253978 94879 3H-QNB 31 Human Binding pKi = 7.9 7.9 -3 5
NoneNone
PDSP KiDatabase 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O None
135398745 2914 3H-NMS 112 Rat Binding pKi = 7.9 7.9 -6 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2914 3H-QNB 112 Rat Binding pKi = 7.9 7.9 -6 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-NMS 112 Rat Binding pKi = 7.9 7.9 -6 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-QNB 112 Rat Binding pKi = 7.9 7.9 -6 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-NMS 112 Rat Binding pKi = 7.9 7.9 -6 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-QNB 112 Rat Binding pKi = 7.9 7.9 -6 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-NMS 112 Rat Binding pKi = 7.9 7.9 -6 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-QNB 112 Rat Binding pKi = 7.9 7.9 -6 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-NMS 112 Rat Binding pKi = 7.9 7.9 -6 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-QNB 112 Rat Binding pKi = 7.9 7.9 -6 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
154825138 216038 3H-NMS 0 Human Binding pKi = 7.9 7.9 1 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
154825138 216038 3H-NMS 0 Rat Binding pKi = 7.9 7.9 -2 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
154734599 2503 3H-NMS 12 Rat Binding pKi = 6.9 6.9 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-NMS 12 Rat Binding pKi = 6.9 6.9 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-NMS 12 Rat Binding pKi = 6.9 6.9 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-NMS 12 Rat Binding pKi = 6.9 6.9 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
279 1661 3H-QNB 26 Human Binding pKi = 7.9 7.9 -2 18
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1661 3H-QNB 26 Human Binding pKi = 7.9 7.9 -2 18
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1661 3H-QNB 26 Human Binding pKi = 7.9 7.9 -2 18
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
2774 3868 3H-NMS 95 Human Binding pKi = 7.9 7.9 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 3868 3H-NMS 95 Human Binding pKi = 7.9 7.9 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593.0 3868 3H-NMS 95 Human Binding pKi = 7.9 7.9 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 3868 3H-NMS 95 Human Binding pKi = 7.9 7.9 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 3868 3H-NMS 95 Human Binding pKi = 7.9 7.9 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 3868 3H-NMS 95 Human Binding pKi = 7.9 7.9 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 3868 3H-NMS 95 Human Binding pKi = 7.9 7.9 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
68617 205527 3H-QNB 62 Human Binding pKi = 5.9 5.9 -20 26
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205527 3H-QNB 62 Human Binding pKi = 5.9 5.9 -20 26
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205527 3H-QNB 62 Human Binding pKi = 5.9 5.9 -20 26
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
154734599 2503 3H-NMS 12 Human Binding pKi = 7.8 7.8 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-NMS 12 Human Binding pKi = 7.8 7.8 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-NMS 12 Human Binding pKi = 7.8 7.8 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-NMS 12 Human Binding pKi = 7.8 7.8 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
1353 1911 3H-QNB 93 Rat Binding pKi = 5.8 5.8 -1047 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 3H-QNB 93 Rat Binding pKi = 5.8 5.8 -1047 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559.0 1911 3H-QNB 93 Rat Binding pKi = 5.8 5.8 -1047 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 3H-QNB 93 Rat Binding pKi = 5.8 5.8 -1047 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 3H-QNB 93 Rat Binding pKi = 5.8 5.8 -1047 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 3H-QNB 93 Rat Binding pKi = 5.8 5.8 -1047 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2726 919 3H-QNB 68 Human Binding pKi = 6.8 6.8 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726.0 919 3H-QNB 68 Human Binding pKi = 6.8 6.8 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 3H-QNB 68 Human Binding pKi = 6.8 6.8 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 3H-QNB 68 Human Binding pKi = 6.8 6.8 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 3H-QNB 68 Human Binding pKi = 6.8 6.8 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 3H-QNB 68 Human Binding pKi = 6.8 6.8 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
242 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795.0 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795.0 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 3H-QNB 124 Human Binding pKi = 5.8 5.8 -67 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
11954259 215979 3H-QNB 0 Human Binding pKi = 5.8 5.8 -13182 43
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
5831 215963 3H-cAMP 0 Human Binding pKi = 5.8 5.8 -25 12
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
5831.0 215963 3H-cAMP 0 Human Binding pKi = 5.8 5.8 -25 12
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
CHEMBL965 215963 3H-cAMP 0 Human Binding pKi = 5.8 5.8 -25 12
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
DB00411 215963 3H-cAMP 0 Human Binding pKi = 5.8 5.8 -25 12
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
310 1922 3H-QNB 0 Human Binding pKi = 7.8 7.8 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
3602 1922 3H-QNB 0 Human Binding pKi = 7.8 7.8 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
CHEMBL3545990 1922 3H-QNB 0 Human Binding pKi = 7.8 7.8 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
154734599 2503 3H-NMS 12 Mouse Binding pKi = 6.8 6.8 -12 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-NMS 12 Mouse Binding pKi = 6.8 6.8 -12 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-NMS 12 Mouse Binding pKi = 6.8 6.8 -12 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-NMS 12 Mouse Binding pKi = 6.8 6.8 -12 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
2995 204405 3H-QNB 53 Human Binding pKi = 6.8 6.8 -4 23
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2995.0 204405 3H-QNB 53 Human Binding pKi = 6.8 6.8 -4 23
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 3H-QNB 53 Human Binding pKi = 6.8 6.8 -4 23
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 3H-QNB 53 Human Binding pKi = 6.8 6.8 -4 23
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
DB01151 204405 3H-QNB 53 Human Binding pKi = 6.8 6.8 -4 23
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2865 4143 3H-QNB 73 Human Binding pKi = 5.8 5.8 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 3H-QNB 73 Human Binding pKi = 5.8 5.8 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 3H-QNB 73 Human Binding pKi = 5.8 5.8 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854.0 4143 3H-QNB 73 Human Binding pKi = 5.8 5.8 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 3H-QNB 73 Human Binding pKi = 5.8 5.8 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 3H-QNB 73 Human Binding pKi = 5.8 5.8 -912 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
135409468 2035 3H-QNB 69 Human Binding pKi = 6.8 6.8 -79 39
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2035 3H-QNB 69 Human Binding pKi = 6.8 6.8 -79 39
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2035 3H-QNB 69 Human Binding pKi = 6.8 6.8 -79 39
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
4601 206747 3H-QNB 35 Human Binding pKi = 6.8 6.8 -1 16
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
4601.0 206747 3H-QNB 35 Human Binding pKi = 6.8 6.8 -1 16
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 206747 3H-QNB 35 Human Binding pKi = 6.8 6.8 -1 16
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 206747 3H-QNB 35 Human Binding pKi = 6.8 6.8 -1 16
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
DB01173 206747 3H-QNB 35 Human Binding pKi = 6.8 6.8 -1 16
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
2448 99323 3H-QNB 70 Human Binding pKi = 5.8 5.8 -70 18
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
2448.0 99323 3H-QNB 70 Human Binding pKi = 5.8 5.8 -70 18
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 99323 3H-QNB 70 Human Binding pKi = 5.8 5.8 -70 18
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
DB12401 99323 3H-QNB 70 Human Binding pKi = 5.8 5.8 -70 18
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
11976 920 3H-QNB 59 Human Binding pKi = 7.7 7.7 -11 24
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 3H-QNB 59 Human Binding pKi = 7.7 7.7 -11 24
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467.0 920 3H-QNB 59 Human Binding pKi = 7.7 7.7 -11 24
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 3H-QNB 59 Human Binding pKi = 7.7 7.7 -11 24
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 3H-QNB 59 Human Binding pKi = 7.7 7.7 -11 24
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
135398737 958 3H-NMS 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 3H-QNB 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-NMS 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-QNB 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-NMS 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-QNB 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-NMS 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-QNB 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-NMS 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-QNB 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-NMS 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-QNB 93 Rat Binding pKi = 7.7 7.7 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
277 1301 3H-QNB 62 Human Binding pKi = 7.7 7.7 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 3H-QNB 62 Human Binding pKi = 7.7 7.7 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913.0 1301 3H-QNB 62 Human Binding pKi = 7.7 7.7 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 3H-QNB 62 Human Binding pKi = 7.7 7.7 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 3H-QNB 62 Human Binding pKi = 7.7 7.7 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 3H-QNB 62 Human Binding pKi = 7.7 7.7 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1712 2492 3H-QNB 43 Human Binding pKi = 7.7 7.7 -3 22
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 3H-QNB 43 Human Binding pKi = 7.7 7.7 -3 22
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078.0 2492 3H-QNB 43 Human Binding pKi = 7.7 7.7 -3 22
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 3H-QNB 43 Human Binding pKi = 7.7 7.7 -3 22
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 3H-QNB 43 Human Binding pKi = 7.7 7.7 -3 22
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 3H-QNB 43 Human Binding pKi = 7.7 7.7 -3 22
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
None 216256 3H-NMS 0 Human Binding pKi = 7.7 7.7 -1 5
NoneNone
PDSP KiDatabase 311 3 1 2 3.9 C1CCC(CC1)C(C#CCN2CCCCC2)(C3=CC=CC=C3)O None
3652 4097 3H-QNB 79 Human Binding pKi = 7.7 7.7 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4097 3H-QNB 79 Human Binding pKi = 7.7 7.7 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4097 3H-QNB 79 Human Binding pKi = 7.7 7.7 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809.0 4097 3H-QNB 79 Human Binding pKi = 7.7 7.7 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4097 3H-QNB 79 Human Binding pKi = 7.7 7.7 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4097 3H-QNB 79 Human Binding pKi = 7.7 7.7 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
11957621 216039 3H-NMS 0 Human Binding pKi = 8.7 8.7 -1 10
NoneNone
PDSP KiDatabase 203 3 2 3 1.3 COC1=C(C=CC(=C1)CCN)O.Cl None
11957621 216039 3H-NMS 0 Rat Binding pKi = 8.7 8.7 -1 10
NoneNone
PDSP KiDatabase 203 3 2 3 1.3 COC1=C(C=CC(=C1)CCN)O.Cl None
1734 116 3H-QNB 10 Human Binding pKi = 8.7 8.7 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-QNB 10 Human Binding pKi = 8.7 8.7 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-QNB 10 Human Binding pKi = 8.7 8.7 -1 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
2381 663 3H-NMS 48 Human Binding pKi = 8.7 8.7 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
2381.0 663 3H-NMS 48 Human Binding pKi = 8.7 8.7 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
374 663 3H-NMS 48 Human Binding pKi = 8.7 8.7 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
7128 663 3H-NMS 48 Human Binding pKi = 8.7 8.7 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
CHEMBL1101 663 3H-NMS 48 Human Binding pKi = 8.7 8.7 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
DB00810 663 3H-NMS 48 Human Binding pKi = 8.7 8.7 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
2381 663 3H-QNB 48 Human Binding pKi = 8.6 8.6 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
2381.0 663 3H-QNB 48 Human Binding pKi = 8.6 8.6 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
374 663 3H-QNB 48 Human Binding pKi = 8.6 8.6 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
7128 663 3H-QNB 48 Human Binding pKi = 8.6 8.6 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
CHEMBL1101 663 3H-QNB 48 Human Binding pKi = 8.6 8.6 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
DB00810 663 3H-QNB 48 Human Binding pKi = 8.6 8.6 -9 8
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
2905 14498 3H-NMS 50 Human Binding pKi = 8.6 8.6 -1 4
NoneNone
PDSP KiDatabase 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 None
2905.0 14498 3H-NMS 50 Human Binding pKi = 8.6 8.6 -1 4
NoneNone
PDSP KiDatabase 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 None
CHEMBL1201338 14498 3H-NMS 50 Human Binding pKi = 8.6 8.6 -1 4
NoneNone
PDSP KiDatabase 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 None
DB00979 14498 3H-NMS 50 Human Binding pKi = 8.6 8.6 -1 4
NoneNone
PDSP KiDatabase 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 None
2745 3861 3H-QNB 42 Human Binding pKi = 8.6 8.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3861 3H-QNB 42 Human Binding pKi = 8.6 8.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572.0 3861 3H-QNB 42 Human Binding pKi = 8.6 8.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3861 3H-QNB 42 Human Binding pKi = 8.6 8.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3861 3H-QNB 42 Human Binding pKi = 8.6 8.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3861 3H-QNB 42 Human Binding pKi = 8.6 8.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3861 3H-QNB 42 Human Binding pKi = 8.6 8.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5387 94879 3H-NMS 31 Human Binding pKi = 8.6 8.6 -3 5
NoneNone
PDSP KiDatabase 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O None
CHEMBL253978 94879 3H-NMS 31 Human Binding pKi = 8.6 8.6 -3 5
NoneNone
PDSP KiDatabase 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O None
154825138 216038 3H-NMS 0 Human Binding pKi = 8.5 8.5 1 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
7534 216373 3H-NMS 0 Human Binding pKi = 6.7 6.7 -2 4
NoneNone
PDSP KiDatabase 291 3 1 4 2.5 CC1CC(CC(N1C)(C)C)OC(=O)C(C2=CC=CC=C2)O None
2200 3131 3H-cAMP 46 Rat Binding pKi = 6.7 6.7 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-cAMP 46 Rat Binding pKi = 6.7 6.7 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-cAMP 46 Rat Binding pKi = 6.7 6.7 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-cAMP 46 Rat Binding pKi = 6.7 6.7 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-cAMP 46 Rat Binding pKi = 6.7 6.7 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-cAMP 46 Rat Binding pKi = 6.7 6.7 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
1613 2348 3H-QNB 53 Human Binding pKi = 5.7 5.7 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 3H-QNB 53 Human Binding pKi = 5.7 5.7 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 3H-QNB 53 Human Binding pKi = 5.7 5.7 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964.0 2348 3H-QNB 53 Human Binding pKi = 5.7 5.7 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 3H-QNB 53 Human Binding pKi = 5.7 5.7 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 3H-QNB 53 Human Binding pKi = 5.7 5.7 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2337 3256 3H-NMS 77 Human Binding pKi = 6.7 6.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 3H-NMS 77 Human Binding pKi = 6.7 6.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 3H-NMS 77 Human Binding pKi = 6.7 6.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 3H-NMS 77 Human Binding pKi = 6.7 6.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 3H-NMS 77 Human Binding pKi = 6.7 6.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 3H-NMS 77 Human Binding pKi = 6.7 6.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
73707487 216374 3H-NMS 0 Human Binding pKi = 7.6 7.6 -1 8
NoneNone
PDSP KiDatabase 355 3 1 4 2.5 CN1C2CCC1CC(C2)OC(=O)C(C3=CC=CC=C3)O.Br None
208 2863 3H-QNB 0 Human Binding pKi = 5.6 5.6 -28 13
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
4541 2863 3H-QNB 0 Human Binding pKi = 5.6 5.6 -28 13
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL1494 2863 3H-QNB 0 Human Binding pKi = 5.6 5.6 -28 13
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2745 3861 3H-NMS 42 Human Binding pKi = 6.6 6.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3861 3H-NMS 42 Human Binding pKi = 6.6 6.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572.0 3861 3H-NMS 42 Human Binding pKi = 6.6 6.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3861 3H-NMS 42 Human Binding pKi = 6.6 6.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3861 3H-NMS 42 Human Binding pKi = 6.6 6.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3861 3H-NMS 42 Human Binding pKi = 6.6 6.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3861 3H-NMS 42 Human Binding pKi = 6.6 6.6 -5 8
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
135398737 958 3H-NMS 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 3H-NMSP 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-NMS 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-NMSP 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-NMS 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-NMSP 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-NMS 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-NMSP 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-NMS 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-NMSP 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-NMS 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-NMSP 93 Human Binding pKi = 7.6 7.6 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2200 3131 3H-QNB 46 Human Binding pKi = 7.6 7.6 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-QNB 46 Human Binding pKi = 7.6 7.6 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-QNB 46 Human Binding pKi = 7.6 7.6 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-QNB 46 Human Binding pKi = 7.6 7.6 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-QNB 46 Human Binding pKi = 7.6 7.6 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-QNB 46 Human Binding pKi = 7.6 7.6 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
135398737 958 3H-QNB 93 Human Binding pKi = 7.5 7.5 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-QNB 93 Human Binding pKi = 7.5 7.5 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-QNB 93 Human Binding pKi = 7.5 7.5 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-QNB 93 Human Binding pKi = 7.5 7.5 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-QNB 93 Human Binding pKi = 7.5 7.5 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-QNB 93 Human Binding pKi = 7.5 7.5 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1209 1658 3H-QNB 75 Human Binding pKi = 5.5 5.5 -23 32
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 3H-QNB 75 Human Binding pKi = 5.5 5.5 -23 32
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 3H-QNB 75 Human Binding pKi = 5.5 5.5 -23 32
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 3H-QNB 75 Human Binding pKi = 5.5 5.5 -23 32
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 3H-QNB 75 Human Binding pKi = 5.5 5.5 -23 32
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2389 3331 3H-QNB 118 Human Binding pKi = 5.5 5.5 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 3H-QNB 118 Human Binding pKi = 5.5 5.5 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 3H-QNB 118 Human Binding pKi = 5.5 5.5 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 3H-QNB 118 Human Binding pKi = 5.5 5.5 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 3H-QNB 118 Human Binding pKi = 5.5 5.5 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 3H-QNB 118 Human Binding pKi = 5.5 5.5 -1445 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
None 216256 3H-NMS 0 Human Binding pKi = 8.5 8.5 -1 5
NoneNone
PDSP KiDatabase 311 3 1 2 3.9 C1CCC(CC1)C(C#CCN2CCCCC2)(C3=CC=CC=C3)O None
130169 3605 3H-NMS 0 Human Binding pKi = 8.5 8.5 -2 5
NoneNone
PDSP KiDatabase 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O None
331 3605 3H-NMS 0 Human Binding pKi = 8.5 8.5 -2 5
NoneNone
PDSP KiDatabase 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O None
2774 3868 3H-QNB 95 Human Binding pKi = 8.5 8.5 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 3868 3H-QNB 95 Human Binding pKi = 8.5 8.5 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593.0 3868 3H-QNB 95 Human Binding pKi = 8.5 8.5 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 3868 3H-QNB 95 Human Binding pKi = 8.5 8.5 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 3868 3H-QNB 95 Human Binding pKi = 8.5 8.5 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 3868 3H-QNB 95 Human Binding pKi = 8.5 8.5 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 3868 3H-QNB 95 Human Binding pKi = 8.5 8.5 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
71128 96810 3H-NMS 25 Human Binding pKi = 8.4 8.4 -30 7
NoneNone
PDSP KiDatabase 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 None
CHEMBL26505 96810 3H-NMS 25 Human Binding pKi = 8.4 8.4 -30 7
NoneNone
PDSP KiDatabase 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 None
1613 2348 3H-QNB 53 Human Binding pKi = 6.5 6.5 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 3H-QNB 53 Human Binding pKi = 6.5 6.5 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 3H-QNB 53 Human Binding pKi = 6.5 6.5 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964.0 2348 3H-QNB 53 Human Binding pKi = 6.5 6.5 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 3H-QNB 53 Human Binding pKi = 6.5 6.5 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 3H-QNB 53 Human Binding pKi = 6.5 6.5 -43 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
15897 2862 3H-QNB 0 Human Binding pKi = 5.5 5.5 -173 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2862 3H-QNB 0 Human Binding pKi = 5.5 5.5 -173 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2862 3H-QNB 0 Human Binding pKi = 5.5 5.5 -173 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
154734599 2503 3H-4-DAMP 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
154734599 2503 3H-NMS 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-4-DAMP 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-NMS 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-4-DAMP 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-NMS 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-4-DAMP 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-NMS 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
None 216257 3H-4-DAMP 0 Human Binding pKi = 7.5 7.5 -1 5
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 216257 3H-NMS 0 Human Binding pKi = 7.5 7.5 -1 5
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
114743 216101 3H-QNB 0 Human Binding pKi = 5.5 5.5 -1 8
NoneNone
PDSP KiDatabase 291 1 1 1 4.9 C1CC(C2=CC=CC=C2C1C3=CC(=C(C=C3)Cl)Cl)N None
135398745 2914 3H-NMS 112 Human Binding pKi = 7.5 7.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2914 3H-NMSP 112 Human Binding pKi = 7.5 7.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-NMS 112 Human Binding pKi = 7.5 7.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-NMSP 112 Human Binding pKi = 7.5 7.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-NMS 112 Human Binding pKi = 7.5 7.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-NMSP 112 Human Binding pKi = 7.5 7.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-NMS 112 Human Binding pKi = 7.5 7.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-NMSP 112 Human Binding pKi = 7.5 7.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-NMS 112 Human Binding pKi = 7.5 7.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-NMSP 112 Human Binding pKi = 7.5 7.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
154734599 2503 3H-QNB 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-QNB 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-QNB 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-QNB 12 Human Binding pKi = 7.5 7.5 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
43815 186920 3H-QNB 64 Human Binding pKi = 6.5 6.5 -8 25
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186920 3H-QNB 64 Human Binding pKi = 6.5 6.5 -8 25
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186920 3H-QNB 64 Human Binding pKi = 6.5 6.5 -8 25
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
2200 3131 3H-NMS 46 Human Binding pKi = 7.5 7.5 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-NMS 46 Human Binding pKi = 7.5 7.5 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-NMS 46 Human Binding pKi = 7.5 7.5 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-NMS 46 Human Binding pKi = 7.5 7.5 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-NMS 46 Human Binding pKi = 7.5 7.5 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-NMS 46 Human Binding pKi = 7.5 7.5 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
310 1922 3H-QNB 0 Human Binding pKi = 7.5 7.5 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
3602 1922 3H-QNB 0 Human Binding pKi = 7.5 7.5 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
CHEMBL3545990 1922 3H-QNB 0 Human Binding pKi = 7.5 7.5 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
2200 3131 3H-NMS 46 Rat Binding pKi = 7.5 7.5 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-NMS 46 Rat Binding pKi = 7.5 7.5 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-NMS 46 Rat Binding pKi = 7.5 7.5 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-NMS 46 Rat Binding pKi = 7.5 7.5 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-NMS 46 Rat Binding pKi = 7.5 7.5 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-NMS 46 Rat Binding pKi = 7.5 7.5 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
3947 206395 3H-QNB 53 Human Binding pKi = 6.5 6.5 -6 16
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
CHEMBL87708 206395 3H-QNB 53 Human Binding pKi = 6.5 6.5 -6 16
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
135398745 2914 35S-GTPGammaS 112 Human Binding pKi = 6.5 6.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 35S-GTPGammaS 112 Human Binding pKi = 6.5 6.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 35S-GTPGammaS 112 Human Binding pKi = 6.5 6.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 35S-GTPGammaS 112 Human Binding pKi = 6.5 6.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 35S-GTPGammaS 112 Human Binding pKi = 6.5 6.5 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 216135 3H-QNB 0 Human Binding pKi = 5.4 5.4 -3801 24
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
2200 3131 3H-NMS 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-NMS 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-NMS 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-NMS 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-NMS 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-NMS 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
154734599 2503 3H-NMS 12 Human Binding pKi = 7.4 7.4 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-NMS 12 Human Binding pKi = 7.4 7.4 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-NMS 12 Human Binding pKi = 7.4 7.4 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-NMS 12 Human Binding pKi = 7.4 7.4 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
2200 3131 3H-4-DAMP 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-4-DAMP 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-4-DAMP 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-4-DAMP 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-4-DAMP 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-4-DAMP 46 Human Binding pKi = 7.4 7.4 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
15897 2862 3H-QNB 0 Human Binding pKi = 5.4 5.4 -173 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2862 3H-QNB 0 Human Binding pKi = 5.4 5.4 -173 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2862 3H-QNB 0 Human Binding pKi = 5.4 5.4 -173 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
2370 623 None 31 Human Binding pKi = 8.4 8.4 -1 5
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
2370.0 623 None 31 Human Binding pKi = 8.4 8.4 -1 5
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
297 623 None 31 Human Binding pKi = 8.4 8.4 -1 5
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
358 623 None 31 Human Binding pKi = 8.4 8.4 -1 5
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
CHEMBL1482 623 None 31 Human Binding pKi = 8.4 8.4 -1 5
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
DB01019 623 None 31 Human Binding pKi = 8.4 8.4 -1 5
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
310 1922 3H-QNB 0 Human Binding pKi = 8.4 8.4 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
3602 1922 3H-QNB 0 Human Binding pKi = 8.4 8.4 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
CHEMBL3545990 1922 3H-QNB 0 Human Binding pKi = 8.4 8.4 -4 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
10938 1702 None 0 Human Binding pKi = 8.4 8.4 -1 4
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
299 1702 None 0 Human Binding pKi = 8.4 8.4 -1 4
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
3256 1702 None 0 Human Binding pKi = 8.4 8.4 -1 4
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
CHEMBL2110739 1702 None 0 Human Binding pKi = 8.4 8.4 -1 4
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
1734 116 3H-QNB 10 Rat Binding pKi = 8.3 8.3 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-QNB 10 Rat Binding pKi = 8.3 8.3 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-QNB 10 Rat Binding pKi = 8.3 8.3 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
4919 206234 3H-NMS 23 Human Binding pKi = 8.3 8.3 -1 8
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
4919.0 206234 3H-NMS 23 Human Binding pKi = 8.3 8.3 -1 8
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 206234 3H-NMS 23 Human Binding pKi = 8.3 8.3 -1 8
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
DB00387 206234 3H-NMS 23 Human Binding pKi = 8.3 8.3 -1 8
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
2726 919 3H-QNB 68 Human Binding pKi = 7.4 7.4 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726.0 919 3H-QNB 68 Human Binding pKi = 7.4 7.4 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 3H-QNB 68 Human Binding pKi = 7.4 7.4 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 3H-QNB 68 Human Binding pKi = 7.4 7.4 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 3H-QNB 68 Human Binding pKi = 7.4 7.4 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 3H-QNB 68 Human Binding pKi = 7.4 7.4 -25 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2200 3131 3H-NMS 46 Mouse Binding pKi = 6.4 6.4 -30 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-NMS 46 Mouse Binding pKi = 6.4 6.4 -30 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-NMS 46 Mouse Binding pKi = 6.4 6.4 -30 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-NMS 46 Mouse Binding pKi = 6.4 6.4 -30 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-NMS 46 Mouse Binding pKi = 6.4 6.4 -30 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-NMS 46 Mouse Binding pKi = 6.4 6.4 -30 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
2774 3868 3H-QNB 95 Human Binding pKi = 7.4 7.4 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 3868 3H-QNB 95 Human Binding pKi = 7.4 7.4 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593.0 3868 3H-QNB 95 Human Binding pKi = 7.4 7.4 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 3868 3H-QNB 95 Human Binding pKi = 7.4 7.4 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 3868 3H-QNB 95 Human Binding pKi = 7.4 7.4 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 3868 3H-QNB 95 Human Binding pKi = 7.4 7.4 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 3868 3H-QNB 95 Human Binding pKi = 7.4 7.4 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
154734599 2503 3H-cAMP 12 Rat Binding pKi = 6.4 6.4 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-cAMP 12 Rat Binding pKi = 6.4 6.4 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-cAMP 12 Rat Binding pKi = 6.4 6.4 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-cAMP 12 Rat Binding pKi = 6.4 6.4 -3 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
1979 77326 3H-cAMP 70 Human Binding pKi = 5.4 5.4 -13 4
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 77326 3H-cAMP 70 Human Binding pKi = 5.4 5.4 -13 4
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
6450478 216012 3H-QNB 0 Human Binding pKi = 6.4 6.4 -10 12
NoneNone
PDSP KiDatabase 340 0 0 6 3.4 CN1CCN(CC1)C2=NC3=CSC=C3C(=CC#N)C4=CSC=C42 None
15387 45822 3H-QNB 55 Human Binding pKi = 5.4 5.4 -22 24
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 3H-QNB 55 Human Binding pKi = 5.4 5.4 -22 24
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
154825138 216038 3H-NMS 0 Rat Binding pKi = 7.3 7.3 -2 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
2200 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
310 1922 3H-cAMP 0 Rat Binding pKi = 7.3 7.3 -10 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
3602 1922 3H-cAMP 0 Rat Binding pKi = 7.3 7.3 -10 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
CHEMBL3545990 1922 3H-cAMP 0 Rat Binding pKi = 7.3 7.3 -10 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
2200 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-NMS 46 Rat Binding pKi = 6.3 6.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
3012003 216145 3H-QNB 0 Human Binding pKi = 6.3 6.3 -2 12
NoneNone
PDSP KiDatabase 311 5 0 3 3.8 CN1CCC(C(C1)COC2=CC=C(C=C2)OC)C3=CC=CC=C3 None
101 3822 3H-QNB 24 Human Binding pKi = 6.3 6.3 -1949 14
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
55752 3822 3H-QNB 24 Human Binding pKi = 6.3 6.3 -1949 14
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL35057 3822 3H-QNB 24 Human Binding pKi = 6.3 6.3 -1949 14
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
3294 2006 None 111 Human Binding pKi = 8.3 8.3 -301 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 None 111 Human Binding pKi = 8.3 8.3 -301 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360.0 2006 None 111 Human Binding pKi = 8.3 8.3 -301 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 None 111 Human Binding pKi = 8.3 8.3 -301 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 None 111 Human Binding pKi = 8.3 8.3 -301 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 None 111 Human Binding pKi = 8.3 8.3 -301 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71202 216372 3H-NMS 0 Human Binding pKi = 8.3 8.3 -1 4
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
66265 94013 None 15 Human Binding pKi = 8.3 8.3 -1 19
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 94013 None 15 Human Binding pKi = 8.3 8.3 -1 19
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
1734 116 3H-NMS 10 Rat Binding pKi = 8.3 8.3 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-NMS 10 Rat Binding pKi = 8.3 8.3 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-NMS 10 Rat Binding pKi = 8.3 8.3 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
2719 917 None 74 Human Binding pKi = 8.3 8.3 -5 11
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
5535 917 None 74 Human Binding pKi = 8.3 8.3 -5 11
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
607 917 None 74 Human Binding pKi = 8.3 8.3 -5 11
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
CHEMBL76 917 None 74 Human Binding pKi = 8.3 8.3 -5 11
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
DB00608 917 None 74 Human Binding pKi = 8.3 8.3 -5 11
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
3652 46244 None 70 Human Binding pKi = 8.3 8.3 -1 9
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
CHEMBL1535 46244 None 70 Human Binding pKi = 8.3 8.3 -1 9
Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
3389 217711 None 0 Human Binding pKi = 8.3 8.3 -1 26
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
15387 45822 None 55 Human Binding pKi = 8.3 8.3 -22 24
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 None 55 Human Binding pKi = 8.3 8.3 -22 24
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
1209 1658 None 75 Human Binding pKi = 8.3 8.3 -23 32
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 None 75 Human Binding pKi = 8.3 8.3 -23 32
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 None 75 Human Binding pKi = 8.3 8.3 -23 32
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 None 75 Human Binding pKi = 8.3 8.3 -23 32
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 None 75 Human Binding pKi = 8.3 8.3 -23 32
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2389 3331 None 118 Human Binding pKi = 8.3 8.3 -1445 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 None 118 Human Binding pKi = 8.3 8.3 -1445 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 None 118 Human Binding pKi = 8.3 8.3 -1445 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 None 118 Human Binding pKi = 8.3 8.3 -1445 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 None 118 Human Binding pKi = 8.3 8.3 -1445 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 None 118 Human Binding pKi = 8.3 8.3 -1445 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5831 215963 None 0 Rat Binding pKi = 8.3 8.3 -1 12
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
5831.0 215963 None 0 Rat Binding pKi = 8.3 8.3 -1 12
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
CHEMBL965 215963 None 0 Rat Binding pKi = 8.3 8.3 -1 12
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
DB00411 215963 None 0 Rat Binding pKi = 8.3 8.3 -1 12
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
187 255 None 39 Human Binding pKi = 8.3 8.3 -6 9
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
187.0 255 None 39 Human Binding pKi = 8.3 8.3 -6 9
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 255 None 39 Human Binding pKi = 8.3 8.3 -6 9
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 255 None 39 Human Binding pKi = 8.3 8.3 -6 9
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 255 None 39 Human Binding pKi = 8.3 8.3 -6 9
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 255 None 39 Human Binding pKi = 8.3 8.3 -6 9
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 255 None 39 Human Binding pKi = 8.3 8.3 -6 9
NoneNone
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
21158560 112793 None 7 Human Binding pKi = 8.3 8.3 -1 4
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 112793 None 7 Human Binding pKi = 8.3 8.3 -1 4
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
1734 116 3H-NMS 10 Mouse Binding pKi = 8.3 8.3 -10 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
1734 116 3H-NMS 10 Rat Binding pKi = 8.3 8.3 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-NMS 10 Mouse Binding pKi = 8.3 8.3 -10 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 3H-NMS 10 Rat Binding pKi = 8.3 8.3 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-NMS 10 Mouse Binding pKi = 8.3 8.3 -10 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 3H-NMS 10 Rat Binding pKi = 8.3 8.3 -3 12
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
441383 20333 None 57 Human Binding pKi = 8.2 8.2 -5 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 20333 None 57 Human Binding pKi = 8.2 8.2 -5 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
2448 99323 None 70 Human Binding pKi = 8.2 8.2 -70 18
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
2448.0 99323 None 70 Human Binding pKi = 8.2 8.2 -70 18
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 99323 None 70 Human Binding pKi = 8.2 8.2 -70 18
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
DB12401 99323 None 70 Human Binding pKi = 8.2 8.2 -70 18
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
107782 14468 None 18 Human Binding pKi = 8.2 8.2 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14468 None 18 Human Binding pKi = 8.2 8.2 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 14468 None 18 Human Binding pKi = 8.2 8.2 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
2812 4779 None 101 Human Binding pKi = 8.2 8.2 -19 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4779 None 101 Human Binding pKi = 8.2 8.2 -19 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
1726 2497 None 13 Rat Binding pKi = 8.2 8.2 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1993 2497 None 13 Rat Binding pKi = 8.2 8.2 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1993.0 2497 None 13 Rat Binding pKi = 8.2 8.2 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
7438 2497 None 13 Rat Binding pKi = 8.2 8.2 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
CHEMBL978 2497 None 13 Rat Binding pKi = 8.2 8.2 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
DB06709 2497 None 13 Rat Binding pKi = 8.2 8.2 -32 5
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1726 2497 None 13 Human Binding pKi = 8.2 8.2 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1993 2497 None 13 Human Binding pKi = 8.2 8.2 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1993.0 2497 None 13 Human Binding pKi = 8.2 8.2 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
7438 2497 None 13 Human Binding pKi = 8.2 8.2 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
CHEMBL978 2497 None 13 Human Binding pKi = 8.2 8.2 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
DB06709 2497 None 13 Human Binding pKi = 8.2 8.2 -12 5
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
212 3806 None 47 Human Binding pKi = 8.2 8.2 -5 25
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 3806 None 47 Human Binding pKi = 8.2 8.2 -5 25
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 3806 None 47 Human Binding pKi = 8.2 8.2 -5 25
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651.0 3806 None 47 Human Binding pKi = 8.2 8.2 -5 25
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 3806 None 47 Human Binding pKi = 8.2 8.2 -5 25
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 3806 None 47 Human Binding pKi = 8.2 8.2 -5 25
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
242 470 None 124 Human Binding pKi = 8.2 8.2 -67 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 None 124 Human Binding pKi = 8.2 8.2 -67 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 None 124 Human Binding pKi = 8.2 8.2 -67 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795.0 470 None 124 Human Binding pKi = 8.2 8.2 -67 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 None 124 Human Binding pKi = 8.2 8.2 -67 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 None 124 Human Binding pKi = 8.2 8.2 -67 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
68617 205527 None 62 Human Binding pKi = 8.2 8.2 -20 26
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205527 None 62 Human Binding pKi = 8.2 8.2 -20 26
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205527 None 62 Human Binding pKi = 8.2 8.2 -20 26
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
2200 3131 3H-NMS 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-NMS 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-NMS 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-NMS 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-NMS 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-NMS 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
154825138 216038 3H-NMS 0 Rat Binding pKi = 7.3 7.3 -2 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
2200 3131 3H-QNB 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-QNB 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-QNB 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-QNB 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-QNB 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-QNB 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
2200 3131 3H-NMS 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-NMS 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-NMS 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-NMS 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-NMS 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-NMS 46 Rat Binding pKi = 7.3 7.3 -7 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
1212 1662 3H-QNB 50 Human Binding pKi = 5.3 5.3 -501 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 3H-QNB 50 Human Binding pKi = 5.3 5.3 -501 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 3H-QNB 50 Human Binding pKi = 5.3 5.3 -501 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372.0 1662 3H-QNB 50 Human Binding pKi = 5.3 5.3 -501 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 3H-QNB 50 Human Binding pKi = 5.3 5.3 -501 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 3H-QNB 50 Human Binding pKi = 5.3 5.3 -501 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2200 3131 3H-QNB 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-QNB 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-QNB 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-QNB 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-QNB 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-QNB 46 Human Binding pKi = 7.3 7.3 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
187 255 3H-NMS 39 Human Binding pKi = 5.3 5.3 -6 9
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
187.0 255 3H-NMS 39 Human Binding pKi = 5.3 5.3 -6 9
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 255 3H-NMS 39 Human Binding pKi = 5.3 5.3 -6 9
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 255 3H-NMS 39 Human Binding pKi = 5.3 5.3 -6 9
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 255 3H-NMS 39 Human Binding pKi = 5.3 5.3 -6 9
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 255 3H-NMS 39 Human Binding pKi = 5.3 5.3 -6 9
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 255 3H-NMS 39 Human Binding pKi = 5.3 5.3 -6 9
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
None 216239 3H-QNB 0 Human Binding pKi = 5.3 5.3 -70794 30
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
2337 3256 3H-QNB 77 Human Binding pKi = 6.3 6.3 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 3H-QNB 77 Human Binding pKi = 6.3 6.3 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 3H-QNB 77 Human Binding pKi = 6.3 6.3 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 3H-QNB 77 Human Binding pKi = 6.3 6.3 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 3H-QNB 77 Human Binding pKi = 6.3 6.3 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 3H-QNB 77 Human Binding pKi = 6.3 6.3 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398737 958 3H-NMS 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 3H-QNB 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-NMS 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-QNB 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-NMS 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-QNB 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-NMS 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-QNB 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-NMS 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-QNB 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-NMS 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-QNB 93 Human Binding pKi = 8.2 8.2 -7 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
154825138 216038 3H-QNB 0 Rat Binding pKi = 8.2 8.2 -2 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
1613 2348 None 53 Human Binding pKi = 8.2 8.2 -43 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 None 53 Human Binding pKi = 8.2 8.2 -43 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 None 53 Human Binding pKi = 8.2 8.2 -43 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964.0 2348 None 53 Human Binding pKi = 8.2 8.2 -43 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 None 53 Human Binding pKi = 8.2 8.2 -43 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 None 53 Human Binding pKi = 8.2 8.2 -43 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
12488 1657 None 56 Human Binding pKi = 8.2 8.2 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 1657 None 56 Human Binding pKi = 8.2 8.2 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 1657 None 56 Human Binding pKi = 8.2 8.2 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 1657 None 56 Human Binding pKi = 8.2 8.2 -12 23
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
1016 3747 None 78 Human Binding pKi = 8.2 8.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pKi = 8.2 8.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pKi = 8.2 8.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pKi = 8.2 8.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pKi = 8.2 8.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 3747 None 78 Human Binding pKi = 8.2 8.2 -12 35
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
154825138 216038 3H-NMS 0 Human Binding pKi = 8.2 8.2 1 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
6918558 14514 None 41 Human Binding pKi = 8.2 8.2 -1 5
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 None
6918558.0 14514 None 41 Human Binding pKi = 8.2 8.2 -1 5
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 None
CHEMBL1201764 14514 None 41 Human Binding pKi = 8.2 8.2 -1 5
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 None
DB06702 14514 None 41 Human Binding pKi = 8.2 8.2 -1 5
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 None
657255 199084 None 34 Human Binding pKi = 8.2 8.2 -9 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 199084 None 34 Human Binding pKi = 8.2 8.2 -9 15
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
103 4153 None 61 Human Binding pKi = 8.2 8.2 -190 53
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 None 61 Human Binding pKi = 8.2 8.2 -190 53
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 None 61 Human Binding pKi = 8.2 8.2 -190 53
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 None 61 Human Binding pKi = 8.2 8.2 -190 53
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 None 61 Human Binding pKi = 8.2 8.2 -190 53
Binding affinity towards human muscarinic receptorBinding affinity towards human muscarinic receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5318 15576 None 49 Human Binding pKi = 8.2 8.2 1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1200348 15576 None 49 Human Binding pKi = 8.2 8.2 1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1221 15576 None 49 Human Binding pKi = 8.2 8.2 1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
3168 9262 None 92 Human Binding pKi = 8.2 8.2 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
3168.0 9262 None 92 Human Binding pKi = 8.2 8.2 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9262 None 92 Human Binding pKi = 8.2 8.2 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
DB00450 9262 None 92 Human Binding pKi = 8.2 8.2 -89 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
2337 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1547484 940 None 74 Human Binding pKi = 8.2 8.2 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
1547484.0 940 None 74 Human Binding pKi = 8.2 8.2 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 940 None 74 Human Binding pKi = 8.2 8.2 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 940 None 74 Human Binding pKi = 8.2 8.2 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 940 None 74 Human Binding pKi = 8.2 8.2 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 940 None 74 Human Binding pKi = 8.2 8.2 -9 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
176 398 None 66 Human Binding pKi = 8.2 8.2 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pKi = 8.2 8.2 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
2157.0 398 None 66 Human Binding pKi = 8.2 8.2 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pKi = 8.2 8.2 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pKi = 8.2 8.2 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 398 None 66 Human Binding pKi = 8.2 8.2 -1 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
4746 204891 None 31 Human Binding pKi = 8.2 8.2 1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
CHEMBL1334033 204891 None 31 Human Binding pKi = 8.2 8.2 1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
CHEMBL75880 204891 None 31 Human Binding pKi = 8.2 8.2 1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
1212 1662 None 50 Human Binding pKi = 8.2 8.2 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 None 50 Human Binding pKi = 8.2 8.2 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 None 50 Human Binding pKi = 8.2 8.2 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372.0 1662 None 50 Human Binding pKi = 8.2 8.2 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 None 50 Human Binding pKi = 8.2 8.2 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 None 50 Human Binding pKi = 8.2 8.2 -501 65
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
124 2981 None 47 Human Binding pKi = 8.2 8.2 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2981 None 47 Human Binding pKi = 8.2 8.2 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2981 None 47 Human Binding pKi = 8.2 8.2 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636.0 2981 None 47 Human Binding pKi = 8.2 8.2 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2981 None 47 Human Binding pKi = 8.2 8.2 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2981 None 47 Human Binding pKi = 8.2 8.2 -77 33
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4189 206922 None 96 Human Binding pKi = 8.2 8.2 -10 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 206922 None 96 Human Binding pKi = 8.2 8.2 -10 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 206922 None 96 Human Binding pKi = 8.2 8.2 -10 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
21855 84246 None 42 Human Binding pKi = 8.2 8.2 -20 6
NoneNone
Drug Central 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 None
21855.0 84246 None 42 Human Binding pKi = 8.2 8.2 -20 6
NoneNone
Drug Central 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 None
CHEMBL22108 84246 None 42 Human Binding pKi = 8.2 8.2 -20 6
NoneNone
Drug Central 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 None
DB08801 84246 None 42 Human Binding pKi = 8.2 8.2 -20 6
NoneNone
Drug Central 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 None
132947 3864 3H-NMS 9 Human Binding pKi = 8.2 8.2 -22 9
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 3864 3H-NMS 9 Human Binding pKi = 8.2 8.2 -22 9
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 3864 3H-NMS 9 Human Binding pKi = 8.2 8.2 -22 9
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
129989 451 3H-NMS 51 Human Binding pKi = 8.2 8.2 -1 9
NoneNone
PDSP KiDatabase 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC None
8584 451 3H-NMS 51 Human Binding pKi = 8.2 8.2 -1 9
NoneNone
PDSP KiDatabase 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC None
CHEMBL43383 451 3H-NMS 51 Human Binding pKi = 8.2 8.2 -1 9
NoneNone
PDSP KiDatabase 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC None
3947 206395 None 53 Human Binding pKi = 8.2 8.2 -6 16
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
CHEMBL87708 206395 None 53 Human Binding pKi = 8.2 8.2 -6 16
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
2200 3131 None 46 Rat Binding pKi = 8.2 8.2 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 None 46 Rat Binding pKi = 8.2 8.2 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 None 46 Rat Binding pKi = 8.2 8.2 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 None 46 Rat Binding pKi = 8.2 8.2 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 None 46 Rat Binding pKi = 8.2 8.2 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 None 46 Rat Binding pKi = 8.2 8.2 -7 12
Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cellsInhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
3198 205513 None 76 Human Binding pKi = 8.2 8.2 -8 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 205513 None 76 Human Binding pKi = 8.2 8.2 -8 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 205513 None 76 Human Binding pKi = 8.2 8.2 -8 34
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
135 2532 None 43 Human Binding pKi = 8.2 8.2 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 None 43 Human Binding pKi = 8.2 8.2 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 None 43 Human Binding pKi = 8.2 8.2 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184.0 2532 None 43 Human Binding pKi = 8.2 8.2 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 None 43 Human Binding pKi = 8.2 8.2 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 None 43 Human Binding pKi = 8.2 8.2 -22 58
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1210 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036.0 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 None 51 Human Binding pKi = 8.2 8.2 -91 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
237 204865 None 48 Human Binding pKi = 8.2 8.2 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 204865 None 48 Human Binding pKi = 8.2 8.2 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 204865 None 48 Human Binding pKi = 8.2 8.2 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 204865 None 48 Human Binding pKi = 8.2 8.2 -1 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
2247 505 None 81 Human Binding pKi = 8.2 8.2 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 None 81 Human Binding pKi = 8.2 8.2 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 505 None 81 Human Binding pKi = 8.2 8.2 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 505 None 81 Human Binding pKi = 8.2 8.2 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 505 None 81 Human Binding pKi = 8.2 8.2 -23 42
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
191 403 None 98 Human Binding pKi = 8.2 8.2 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 None 98 Human Binding pKi = 8.2 8.2 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 None 98 Human Binding pKi = 8.2 8.2 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170.0 403 None 98 Human Binding pKi = 8.2 8.2 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 None 98 Human Binding pKi = 8.2 8.2 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 None 98 Human Binding pKi = 8.2 8.2 -29 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
1548955 88581 None 20 Human Binding pKi = 8.2 8.2 -1 18
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 88581 None 20 Human Binding pKi = 8.2 8.2 -1 18
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 88581 None 20 Human Binding pKi = 8.2 8.2 -1 18
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
60838 183874 None 99 Human Binding pKi = 8.2 8.2 1 2
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC None
CHEMBL481 183874 None 99 Human Binding pKi = 8.2 8.2 1 2
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 586 4 1 9 4.1 CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC None
4735 195115 None 96 Human Binding pKi = 8.2 8.2 -6 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
CHEMBL361506 195115 None 96 Human Binding pKi = 8.2 8.2 -6 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
CHEMBL55 195115 None 96 Human Binding pKi = 8.2 8.2 -6 10
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
2274 3173 None 58 Human Binding pKi = 8.2 8.2 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 None 58 Human Binding pKi = 8.2 8.2 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917.0 3173 None 58 Human Binding pKi = 8.2 8.2 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 None 58 Human Binding pKi = 8.2 8.2 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 None 58 Human Binding pKi = 8.2 8.2 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 None 58 Human Binding pKi = 8.2 8.2 -16 31
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
154059 3637 None 51 Human Binding pKi = 8.2 8.2 -5 8
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
154059.0 3637 None 51 Human Binding pKi = 8.2 8.2 -5 8
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
2457 3637 None 51 Human Binding pKi = 8.2 8.2 -5 8
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
7483 3637 None 51 Human Binding pKi = 8.2 8.2 -5 8
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
CHEMBL1734 3637 None 51 Human Binding pKi = 8.2 8.2 -5 8
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
DB01591 3637 None 51 Human Binding pKi = 8.2 8.2 -5 8
NoneNone
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
2995 204405 None 53 Human Binding pKi = 8.2 8.2 -4 23
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2995.0 204405 None 53 Human Binding pKi = 8.2 8.2 -4 23
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 None 53 Human Binding pKi = 8.2 8.2 -4 23
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 None 53 Human Binding pKi = 8.2 8.2 -4 23
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
DB01151 204405 None 53 Human Binding pKi = 8.2 8.2 -4 23
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
11057 176149 None 23 Human Binding pKi = 8.2 8.2 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 176149 None 23 Human Binding pKi = 8.2 8.2 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 176149 None 23 Human Binding pKi = 8.2 8.2 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 176149 None 23 Human Binding pKi = 8.2 8.2 1 20
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
6726 1280 None 51 Human Binding pKi = 8.2 8.2 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
6726.0 1280 None 51 Human Binding pKi = 8.2 8.2 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
7151 1280 None 51 Human Binding pKi = 8.2 8.2 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
749 1280 None 51 Human Binding pKi = 8.2 8.2 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL648 1280 None 51 Human Binding pKi = 8.2 8.2 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB01176 1280 None 51 Human Binding pKi = 8.2 8.2 -5 13
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
3191 102858 None 97 Human Binding pKi = 8.2 8.2 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
3191.0 102858 None 97 Human Binding pKi = 8.2 8.2 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 102858 None 97 Human Binding pKi = 8.2 8.2 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
DB11742 102858 None 97 Human Binding pKi = 8.2 8.2 -5 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
4976 203579 None 29 Human Binding pKi = 8.2 8.2 -1 12
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
CHEMBL668 203579 None 29 Human Binding pKi = 8.2 8.2 -1 12
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
1224 1432 None 83 Human Binding pKi = 8.2 8.2 -3 13
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 None 83 Human Binding pKi = 8.2 8.2 -3 13
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100.0 1432 None 83 Human Binding pKi = 8.2 8.2 -3 13
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 None 83 Human Binding pKi = 8.2 8.2 -3 13
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 None 83 Human Binding pKi = 8.2 8.2 -3 13
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 None 83 Human Binding pKi = 8.2 8.2 -3 13
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 None 83 Human Binding pKi = 8.2 8.2 -3 13
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1427 2013 None 54 Human Binding pKi = 8.2 8.2 -2 27
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 None 54 Human Binding pKi = 8.2 8.2 -2 27
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 None 54 Human Binding pKi = 8.2 8.2 -2 27
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 None 54 Human Binding pKi = 8.2 8.2 -2 27
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 None 54 Human Binding pKi = 8.2 8.2 -2 27
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
2230 465 3H-QNB 60 Human Binding pKi = 7.2 7.2 -218 10
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
296 465 3H-QNB 60 Human Binding pKi = 7.2 7.2 -218 10
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
CHEMBL7303 465 3H-QNB 60 Human Binding pKi = 7.2 7.2 -218 10
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
DB04365 465 3H-QNB 60 Human Binding pKi = 7.2 7.2 -218 10
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
154825138 216038 3H-NMS 0 Mouse Binding pKi = 7.2 7.2 -7 11
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
20980871 216430 3H-QNB 0 Human Binding pKi = 7.2 7.2 -15 8
NoneNone
PDSP KiDatabase 295 3 0 2 4.7 CN(C)CCC=C1C2=CC=CC=C2CSC3=CC=CC=C31 None
3155.0 216430 3H-QNB 0 Human Binding pKi = 7.2 7.2 -15 8
NoneNone
PDSP KiDatabase 295 3 0 2 4.7 CN(C)CCC=C1C2=CC=CC=C2CSC3=CC=CC=C31 None
CHEMBL108947 216430 3H-QNB 0 Human Binding pKi = 7.2 7.2 -15 8
NoneNone
PDSP KiDatabase 295 3 0 2 4.7 CN(C)CCC=C1C2=CC=CC=C2CSC3=CC=CC=C31 None
CHEMBL1492500 216430 3H-QNB 0 Human Binding pKi = 7.2 7.2 -15 8
NoneNone
PDSP KiDatabase 295 3 0 2 4.7 CN(C)CCC=C1C2=CC=CC=C2CSC3=CC=CC=C31 None
DB09167 216430 3H-QNB 0 Human Binding pKi = 7.2 7.2 -15 8
NoneNone
PDSP KiDatabase 295 3 0 2 4.7 CN(C)CCC=C1C2=CC=CC=C2CSC3=CC=CC=C31 None
2200 3131 3H-NMS 46 Human Binding pKi = 7.2 7.2 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 3H-NMS 46 Human Binding pKi = 7.2 7.2 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 3H-NMS 46 Human Binding pKi = 7.2 7.2 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 3H-NMS 46 Human Binding pKi = 7.2 7.2 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 3H-NMS 46 Human Binding pKi = 7.2 7.2 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 3H-NMS 46 Human Binding pKi = 7.2 7.2 -2 12
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4839 216375 3H-NMS 0 Human Binding pKi = 7.2 7.2 1 4
NoneNone
PDSP KiDatabase 323 5 0 3 3.8 CCN1CCCC(C1)OC(=O)C(C2=CC=CC=C2)C3=CC=CC=C3 None
154734599 2503 3H-QNB 12 Human Binding pKi = 7.2 7.2 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-QNB 12 Human Binding pKi = 7.2 7.2 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-QNB 12 Human Binding pKi = 7.2 7.2 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-QNB 12 Human Binding pKi = 7.2 7.2 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
2337 3256 3H-QNB 77 Human Binding pKi = 6.2 6.2 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3256 3H-NMS 77 Rat Binding pKi = 6.2 6.2 -74 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 3H-QNB 77 Human Binding pKi = 6.2 6.2 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 3H-NMS 77 Rat Binding pKi = 6.2 6.2 -74 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 3H-QNB 77 Human Binding pKi = 6.2 6.2 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 3H-NMS 77 Rat Binding pKi = 6.2 6.2 -74 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 3H-QNB 77 Human Binding pKi = 6.2 6.2 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 3H-NMS 77 Rat Binding pKi = 6.2 6.2 -74 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 3H-QNB 77 Human Binding pKi = 6.2 6.2 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 3H-NMS 77 Rat Binding pKi = 6.2 6.2 -74 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 3H-QNB 77 Human Binding pKi = 6.2 6.2 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 3H-NMS 77 Rat Binding pKi = 6.2 6.2 -74 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5387 94879 3H-QNB 31 Rat Binding pKi = 7.2 7.2 -22 5
NoneNone
PDSP KiDatabase 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O None
CHEMBL253978 94879 3H-QNB 31 Rat Binding pKi = 7.2 7.2 -22 5
NoneNone
PDSP KiDatabase 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O None
3337 206367 3H-QNB 27 Human Binding pKi = 5.2 5.2 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337.0 206367 3H-QNB 27 Human Binding pKi = 5.2 5.2 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 3H-QNB 27 Human Binding pKi = 5.2 5.2 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 3H-QNB 27 Human Binding pKi = 5.2 5.2 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 3H-QNB 27 Human Binding pKi = 5.2 5.2 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 3H-QNB 27 Human Binding pKi = 5.2 5.2 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206367 3H-QNB 27 Human Binding pKi = 5.2 5.2 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
4919 206234 3H-QNB 23 Human Binding pKi = 8.2 8.2 -1 8
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
4919.0 206234 3H-QNB 23 Human Binding pKi = 8.2 8.2 -1 8
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 206234 3H-QNB 23 Human Binding pKi = 8.2 8.2 -1 8
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
DB00387 206234 3H-QNB 23 Human Binding pKi = 8.2 8.2 -1 8
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
4212 198679 None 82 Human Binding pKi = 8.2 8.2 -1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 None
CHEMBL1417019 198679 None 82 Human Binding pKi = 8.2 8.2 -1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 None
CHEMBL58 198679 None 82 Human Binding pKi = 8.2 8.2 -1 4
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 None
1530 2182 None 50 Human Binding pKi = 8.2 8.2 -32 21
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2182 None 50 Human Binding pKi = 8.2 8.2 -32 21
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827.0 2182 None 50 Human Binding pKi = 8.2 8.2 -32 21
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2182 None 50 Human Binding pKi = 8.2 8.2 -32 21
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2182 None 50 Human Binding pKi = 8.2 8.2 -32 21
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2182 None 50 Human Binding pKi = 8.2 8.2 -32 21
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
1971 2866 None 38 Human Binding pKi = 8.2 8.2 -3 30
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 None 38 Human Binding pKi = 8.2 8.2 -3 30
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 None 38 Human Binding pKi = 8.2 8.2 -3 30
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543.0 2866 None 38 Human Binding pKi = 8.2 8.2 -3 30
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 None 38 Human Binding pKi = 8.2 8.2 -3 30
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 None 38 Human Binding pKi = 8.2 8.2 -3 30
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
1225 1471 None 26 Human Binding pKi = 8.2 8.2 -85 22
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 None 26 Human Binding pKi = 8.2 8.2 -85 22
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667468.0 1471 None 26 Human Binding pKi = 8.2 8.2 -85 22
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 None 26 Human Binding pKi = 8.2 8.2 -85 22
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477.0 1471 None 26 Human Binding pKi = 8.2 8.2 -85 22
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL101740 1471 None 26 Human Binding pKi = 8.2 8.2 -85 22
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 None 26 Human Binding pKi = 8.2 8.2 -85 22
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 None 26 Human Binding pKi = 8.2 8.2 -85 22
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
2200 3131 None 46 Human Binding pKi = 8.2 8.2 -2 12
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3131 None 46 Human Binding pKi = 8.2 8.2 -2 12
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3131 None 46 Human Binding pKi = 8.2 8.2 -2 12
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848.0 3131 None 46 Human Binding pKi = 8.2 8.2 -2 12
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3131 None 46 Human Binding pKi = 8.2 8.2 -2 12
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3131 None 46 Human Binding pKi = 8.2 8.2 -2 12
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
3652 4097 None 79 Human Binding pKi = 8.2 8.2 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4097 None 79 Human Binding pKi = 8.2 8.2 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4097 None 79 Human Binding pKi = 8.2 8.2 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809.0 4097 None 79 Human Binding pKi = 8.2 8.2 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4097 None 79 Human Binding pKi = 8.2 8.2 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4097 None 79 Human Binding pKi = 8.2 8.2 -3 18
Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
180 401 3H-QNB 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 3H-QNB 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 3H-QNB 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160.0 401 3H-QNB 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 3H-QNB 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 3H-QNB 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
5284550 41721 None 15 Human Binding pKi = 8.1 8.1 -1 9
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
5284550.0 41721 None 15 Human Binding pKi = 8.1 8.1 -1 9
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
CHEMBL108947 41721 None 15 Human Binding pKi = 8.1 8.1 -1 9
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
CHEMBL1492500 41721 None 15 Human Binding pKi = 8.1 8.1 -1 9
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
DB09167 41721 None 15 Human Binding pKi = 8.1 8.1 -1 9
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
4011 82408 None 49 Human Binding pKi = 8.1 8.1 -11 24
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 82408 None 49 Human Binding pKi = 8.1 8.1 -11 24
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
2284 3182 None 33 Human Binding pKi = 8.1 8.1 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3182 None 33 Human Binding pKi = 8.1 8.1 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3182 None 33 Human Binding pKi = 8.1 8.1 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3182 None 33 Human Binding pKi = 8.1 8.1 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3182 None 33 Human Binding pKi = 8.1 8.1 -7 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2726 919 None 68 Human Binding pKi = 8.1 8.1 -25 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726.0 919 None 68 Human Binding pKi = 8.1 8.1 -25 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 None 68 Human Binding pKi = 8.1 8.1 -25 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 None 68 Human Binding pKi = 8.1 8.1 -25 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 None 68 Human Binding pKi = 8.1 8.1 -25 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 None 68 Human Binding pKi = 8.1 8.1 -25 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
3055 1433 None 44 Human Binding pKi = 8.1 8.1 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
313 1433 None 44 Human Binding pKi = 8.1 8.1 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
7163 1433 None 44 Human Binding pKi = 8.1 8.1 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
CHEMBL936 1433 None 44 Human Binding pKi = 8.1 8.1 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
DB01231 1433 None 44 Human Binding pKi = 8.1 8.1 -1 9
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
2335 11848 None 22 Human Binding pKi = 8.1 8.1 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 11848 None 22 Human Binding pKi = 8.1 8.1 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 11848 None 22 Human Binding pKi = 8.1 8.1 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 11848 None 22 Human Binding pKi = 8.1 8.1 1 12
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
43815 186920 None 64 Human Binding pKi = 8.1 8.1 -8 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 186920 None 64 Human Binding pKi = 8.1 8.1 -8 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 186920 None 64 Human Binding pKi = 8.1 8.1 -8 25
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
5831 215963 3H-QNB 0 Human Binding pKi = 8.1 8.1 -25 12
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
5831.0 215963 3H-QNB 0 Human Binding pKi = 8.1 8.1 -25 12
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
CHEMBL965 215963 3H-QNB 0 Human Binding pKi = 8.1 8.1 -25 12
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
DB00411 215963 3H-QNB 0 Human Binding pKi = 8.1 8.1 -25 12
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
135398745 2914 None 112 Human Binding pKi = 8.1 8.1 -32 65
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 None 112 Human Binding pKi = 8.1 8.1 -32 65
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 None 112 Human Binding pKi = 8.1 8.1 -32 65
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 None 112 Human Binding pKi = 8.1 8.1 -32 65
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 None 112 Human Binding pKi = 8.1 8.1 -32 65
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
124087 1389 None 114 Human Binding pKi = 8.1 8.1 -7 15
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
124087.0 1389 None 114 Human Binding pKi = 8.1 8.1 -7 15
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 1389 None 114 Human Binding pKi = 8.1 8.1 -7 15
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 1389 None 114 Human Binding pKi = 8.1 8.1 -7 15
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 1389 None 114 Human Binding pKi = 8.1 8.1 -7 15
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 1389 None 114 Human Binding pKi = 8.1 8.1 -7 15
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
6075 150108 None 42 Human Binding pKi = 8.1 8.1 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 150108 None 42 Human Binding pKi = 8.1 8.1 -2 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
1712 2492 None 43 Human Binding pKi = 8.1 8.1 -3 22
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 None 43 Human Binding pKi = 8.1 8.1 -3 22
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078.0 2492 None 43 Human Binding pKi = 8.1 8.1 -3 22
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 None 43 Human Binding pKi = 8.1 8.1 -3 22
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 None 43 Human Binding pKi = 8.1 8.1 -3 22
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 None 43 Human Binding pKi = 8.1 8.1 -3 22
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4601 206747 None 35 Human Binding pKi = 8.1 8.1 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
4601.0 206747 None 35 Human Binding pKi = 8.1 8.1 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 206747 None 35 Human Binding pKi = 8.1 8.1 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 206747 None 35 Human Binding pKi = 8.1 8.1 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
DB01173 206747 None 35 Human Binding pKi = 8.1 8.1 -1 16
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
42470 216183 3H-cAMP 0 Rat Binding pKi = 8.1 8.1 -15 5
NoneNone
PDSP KiDatabase 345 10 0 3 4.9 CCN(CCCC(=O)C1CCCCC1)C(C)CC2=CC=C(C=C2)OC None
73707487 216374 None 0 Human Binding pKi = 8.1 8.1 -1 8
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
2398 954 None 62 Human Binding pKi = 8.1 8.1 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 954 None 62 Human Binding pKi = 8.1 8.1 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801.0 954 None 62 Human Binding pKi = 8.1 8.1 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 954 None 62 Human Binding pKi = 8.1 8.1 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 954 None 62 Human Binding pKi = 8.1 8.1 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 954 None 62 Human Binding pKi = 8.1 8.1 -1 29
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
62865 1274 None 0 Human Binding pKi = 8.1 8.1 -3 14
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 1274 None 0 Human Binding pKi = 8.1 8.1 -3 14
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 1274 None 0 Human Binding pKi = 8.1 8.1 -3 14
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 1274 None 0 Human Binding pKi = 8.1 8.1 -3 14
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 1274 None 0 Human Binding pKi = 8.1 8.1 -3 14
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
3337 206367 3H-QNB 27 Human Binding pKi = 5.1 5.1 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337.0 206367 3H-QNB 27 Human Binding pKi = 5.1 5.1 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 3H-QNB 27 Human Binding pKi = 5.1 5.1 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 3H-QNB 27 Human Binding pKi = 5.1 5.1 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 3H-QNB 27 Human Binding pKi = 5.1 5.1 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 3H-QNB 27 Human Binding pKi = 5.1 5.1 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206367 3H-QNB 27 Human Binding pKi = 5.1 5.1 -190 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
154734599 2503 3H-QNB 12 Human Binding pKi = 7.1 7.1 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-QNB 12 Human Binding pKi = 7.1 7.1 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-QNB 12 Human Binding pKi = 7.1 7.1 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-QNB 12 Human Binding pKi = 7.1 7.1 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
2337 3256 3H-QNB 77 Human Binding pKi = 6.1 6.1 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 3H-QNB 77 Human Binding pKi = 6.1 6.1 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 3H-QNB 77 Human Binding pKi = 6.1 6.1 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 3H-QNB 77 Human Binding pKi = 6.1 6.1 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 3H-QNB 77 Human Binding pKi = 6.1 6.1 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 3H-QNB 77 Human Binding pKi = 6.1 6.1 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
103 4153 3H-QNB 61 Human Binding pKi = 7.1 7.1 -190 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 3H-QNB 61 Human Binding pKi = 7.1 7.1 -190 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 3H-QNB 61 Human Binding pKi = 7.1 7.1 -190 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 3H-QNB 61 Human Binding pKi = 7.1 7.1 -190 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 3H-QNB 61 Human Binding pKi = 7.1 7.1 -190 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
310 1922 3H-QNB 0 Rat Binding pKi = 7.1 7.1 -10 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
3602 1922 3H-QNB 0 Rat Binding pKi = 7.1 7.1 -10 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
CHEMBL3545990 1922 3H-QNB 0 Rat Binding pKi = 7.1 7.1 -10 10
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
277 1301 3H-QNB 62 Human Binding pKi = 8.1 8.1 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 3H-QNB 62 Human Binding pKi = 8.1 8.1 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913.0 1301 3H-QNB 62 Human Binding pKi = 8.1 8.1 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 3H-QNB 62 Human Binding pKi = 8.1 8.1 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 3H-QNB 62 Human Binding pKi = 8.1 8.1 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 3H-QNB 62 Human Binding pKi = 8.1 8.1 -8 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
100 3805 None 58 Human Binding pKi = 8.1 8.1 -14 55
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 None 58 Human Binding pKi = 8.1 8.1 -14 55
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 None 58 Human Binding pKi = 8.1 8.1 -14 55
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 None 58 Human Binding pKi = 8.1 8.1 -14 55
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 None 58 Human Binding pKi = 8.1 8.1 -14 55
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
319 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
321 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
444031 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
444031.0 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
784 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
CHEMBL1346 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
DB00496 1324 None 44 Human Binding pKi = 8.1 8.1 -9 9
GRAC: human M4 antagonistGRAC: human M4 antagonist
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
154734599 2503 3H-NMS 12 Human Binding pKi = 8.1 8.1 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2503 3H-NMS 12 Human Binding pKi = 8.1 8.1 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2503 3H-NMS 12 Human Binding pKi = 8.1 8.1 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2503 3H-NMS 12 Human Binding pKi = 8.1 8.1 -2 11
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
180 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160.0 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
4919 206234 None 23 Human Binding pKi = 8.1 8.1 -1 8
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
4919.0 206234 None 23 Human Binding pKi = 8.1 8.1 -1 8
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 206234 None 23 Human Binding pKi = 8.1 8.1 -1 8
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
DB00387 206234 None 23 Human Binding pKi = 8.1 8.1 -1 8
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
1371 1923 None 11 Human Binding pKi = 8.1 8.1 -1 5
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
24199 1923 None 11 Human Binding pKi = 8.1 8.1 -1 5
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
24199.0 1923 None 11 Human Binding pKi = 8.1 8.1 -1 5
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
323 1923 None 11 Human Binding pKi = 8.1 8.1 -1 5
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
CHEMBL1201325 1923 None 11 Human Binding pKi = 8.1 8.1 -1 5
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
DB06787 1923 None 11 Human Binding pKi = 8.1 8.1 -1 5
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
2774 3868 3H-NMS 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 3868 3H-NMS 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593.0 3868 3H-NMS 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 3868 3H-NMS 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 3868 3H-NMS 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 3868 3H-NMS 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 3868 3H-NMS 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5648 78411 None 9 Human Binding pKi = 8.1 8.1 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 78411 None 9 Human Binding pKi = 8.1 8.1 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 78411 None 9 Human Binding pKi = 8.1 8.1 -1 5
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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
2028 2979 None 80 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2979 None 80 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2979 None 80 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634.0 2979 None 80 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2979 None 80 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2979 None 80 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
2774 3868 None 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 3868 None 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593.0 3868 None 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 3868 None 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 3868 None 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 3868 None 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 3868 None 95 Human Binding pKi = 8.1 8.1 1 9
NoneNone
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
2705 3842 None 64 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
360 3842 None 64 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
443879 3842 None 64 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
443879.0 3842 None 64 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
CHEMBL1382 3842 None 64 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
DB01036 3842 None 64 Human Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
2705 3842 None 64 Rat Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
360 3842 None 64 Rat Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
443879 3842 None 64 Rat Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
443879.0 3842 None 64 Rat Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
CHEMBL1382 3842 None 64 Rat Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
DB01036 3842 None 64 Rat Binding pKi = 8.1 8.1 -1 10
Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
26987 949 None 33 Human Binding pKi = 8.1 8.1 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
26987.0 949 None 33 Human Binding pKi = 8.1 8.1 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 949 None 33 Human Binding pKi = 8.1 8.1 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 949 None 33 Human Binding pKi = 8.1 8.1 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 949 None 33 Human Binding pKi = 8.1 8.1 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 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 949 None 33 Human Binding pKi = 8.1 8.1 -38 21
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
4904 155521 None 48 Human Binding pKi = 8.1 8.1 -1 5
NoneNone
Drug Central 295 5 1 2 3.8 OC(CCN1CCCCC1)(c1ccccc1)c1ccccc1 None
CHEMBL404215 155521 None 48 Human Binding pKi = 8.1 8.1 -1 5
NoneNone
Drug Central 295 5 1 2 3.8 OC(CCN1CCCCC1)(c1ccccc1)c1ccccc1 None
72054.0 216228 3H-NMS 0 Human Binding pKi = 8.1 8.1 -10 6
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
CHEMBL1346 216228 3H-NMS 0 Human Binding pKi = 8.1 8.1 -10 6
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
DB00496 216228 3H-NMS 0 Human Binding pKi = 8.1 8.1 -10 6
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
277 1301 None 62 Human Binding pKi = 8.1 8.1 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 None 62 Human Binding pKi = 8.1 8.1 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913.0 1301 None 62 Human Binding pKi = 8.1 8.1 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 None 62 Human Binding pKi = 8.1 8.1 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 None 62 Human Binding pKi = 8.1 8.1 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 None 62 Human Binding pKi = 8.1 8.1 -8 50
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1201549 597 None 24 Human Binding pKi = 8.1 8.1 -1 20
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
1201549.0 597 None 24 Human Binding pKi = 8.1 8.1 -1 20
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 597 None 24 Human Binding pKi = 8.1 8.1 -1 20
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 597 None 24 Human Binding pKi = 8.1 8.1 -1 20
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 597 None 24 Human Binding pKi = 8.1 8.1 -1 20
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 597 None 24 Human Binding pKi = 8.1 8.1 -1 20
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 597 None 24 Human Binding pKi = 8.1 8.1 -1 20
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
2286 3183 None 51 Human Binding pKi = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 None 51 Human Binding pKi = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927.0 3183 None 51 Human Binding pKi = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 None 51 Human Binding pKi = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 None 51 Human Binding pKi = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 None 51 Human Binding pKi = 8.1 8.1 1 30
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4601 206747 3H-NMS 35 Human Binding pKi = 7.1 7.1 -1 16
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
4601.0 206747 3H-NMS 35 Human Binding pKi = 7.1 7.1 -1 16
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 206747 3H-NMS 35 Human Binding pKi = 7.1 7.1 -1 16
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 206747 3H-NMS 35 Human Binding pKi = 7.1 7.1 -1 16
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
DB01173 206747 3H-NMS 35 Human Binding pKi = 7.1 7.1 -1 16
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
1225 1471 3H-QNB 26 Human Binding pKi = 7.1 7.1 -85 22
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 3H-QNB 26 Human Binding pKi = 7.1 7.1 -85 22
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667468.0 1471 3H-QNB 26 Human Binding pKi = 7.1 7.1 -85 22
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 3H-QNB 26 Human Binding pKi = 7.1 7.1 -85 22
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477.0 1471 3H-QNB 26 Human Binding pKi = 7.1 7.1 -85 22
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL101740 1471 3H-QNB 26 Human Binding pKi = 7.1 7.1 -85 22
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 3H-QNB 26 Human Binding pKi = 7.1 7.1 -85 22
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 3H-QNB 26 Human Binding pKi = 7.1 7.1 -85 22
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
1615 167791 3H-QNB 24 Human Binding pKi = 5.1 5.1 -22 44
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167791 3H-QNB 24 Human Binding pKi = 5.1 5.1 -22 44
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
3294 2006 3H-NMS 111 Human Binding pKi = 5.1 5.1 -301 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 3H-NMS 111 Human Binding pKi = 5.1 5.1 -301 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360.0 2006 3H-NMS 111 Human Binding pKi = 5.1 5.1 -301 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 3H-NMS 111 Human Binding pKi = 5.1 5.1 -301 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 3H-NMS 111 Human Binding pKi = 5.1 5.1 -301 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 3H-NMS 111 Human Binding pKi = 5.1 5.1 -301 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1971 2866 3H-QNB 38 Human Binding pKi = 7.1 7.1 -3 30
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 3H-QNB 38 Human Binding pKi = 7.1 7.1 -3 30
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 3H-QNB 38 Human Binding pKi = 7.1 7.1 -3 30
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543.0 2866 3H-QNB 38 Human Binding pKi = 7.1 7.1 -3 30
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 3H-QNB 38 Human Binding pKi = 7.1 7.1 -3 30
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 3H-QNB 38 Human Binding pKi = 7.1 7.1 -3 30
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
100 3805 3H-QNB 58 Human Binding pKi = 8.1 8.1 -14 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 3H-QNB 58 Human Binding pKi = 8.1 8.1 -14 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 3H-QNB 58 Human Binding pKi = 8.1 8.1 -14 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 3H-QNB 58 Human Binding pKi = 8.1 8.1 -14 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 3H-QNB 58 Human Binding pKi = 8.1 8.1 -14 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
11693 1827 None 16 Human Binding pKi = 8.0 8.0 1 5
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
3494 1827 None 16 Human Binding pKi = 8.0 8.0 1 5
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
3494.0 1827 None 16 Human Binding pKi = 8.0 8.0 1 5
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
4302 1827 None 16 Human Binding pKi = 8.0 8.0 1 5
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
7459 1827 None 16 Human Binding pKi = 8.0 8.0 1 5
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
9933193.0 1827 None 16 Human Binding pKi = 8.0 8.0 1 5
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
CHEMBL1201335 1827 None 16 Human Binding pKi = 8.0 8.0 1 5
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
DB00986 1827 None 16 Human Binding pKi = 8.0 8.0 1 5
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
25897919 55652 None 14 Human Binding pKi = 8.0 8.0 -3 8
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
657308.0 55652 None 14 Human Binding pKi = 8.0 8.0 -3 8
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 55652 None 14 Human Binding pKi = 8.0 8.0 -3 8
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 55652 None 14 Human Binding pKi = 8.0 8.0 -3 8
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 55652 None 14 Human Binding pKi = 8.0 8.0 -3 8
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
DB00332 55652 None 14 Human Binding pKi = 8.0 8.0 -3 8
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
10129 3322 None 0 Human Binding pKi = 8.0 8.0 -1 5
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 3322 None 0 Human Binding pKi = 8.0 8.0 -1 5
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
11753673.0 3322 None 0 Human Binding pKi = 8.0 8.0 -1 5
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 3322 None 0 Human Binding pKi = 8.0 8.0 -1 5
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 3322 None 0 Human Binding pKi = 8.0 8.0 -1 5
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 3322 None 0 Human Binding pKi = 8.0 8.0 -1 5
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
12057539 208041 None 42 Rat Binding pKi = 8.0 8.0 -5 20
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 None 42 Rat Binding pKi = 8.0 8.0 -5 20
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 None 42 Rat Binding pKi = 8.0 8.0 -5 20
Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
11968014 12758 None 5 Human Binding pKi = 8.0 8.0 -12 9
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
119680147.0 12758 None 5 Human Binding pKi = 8.0 8.0 -12 9
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 12758 None 5 Human Binding pKi = 8.0 8.0 -12 9
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
DB00747 12758 None 5 Human Binding pKi = 8.0 8.0 -12 9
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
3042 1414 None 35 Human Binding pKi = 8.0 8.0 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
3042.0 1414 None 35 Human Binding pKi = 8.0 8.0 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1414 None 35 Human Binding pKi = 8.0 8.0 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1414 None 35 Human Binding pKi = 8.0 8.0 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1414 None 35 Human Binding pKi = 8.0 8.0 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1414 None 35 Human Binding pKi = 8.0 8.0 -1 14
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
12057539 208041 None 42 Human Binding pKi = 8.0 8.0 -1 20
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 None 42 Human Binding pKi = 8.0 8.0 -1 20
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 None 42 Human Binding pKi = 8.0 8.0 -1 20
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
2039 2982 None 19 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
5749 2982 None 19 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
5749.0 2982 None 19 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
7257 2982 None 19 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
CHEMBL1201286 2982 None 19 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
DB00219 2982 None 19 Human Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C None
154417 23181 None 60 Human Binding pKi = 8 8.0 -1 5
NoneNone
Drug Central 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 None
CHEMBL1331216 23181 None 60 Human Binding pKi = 8 8.0 -1 5
NoneNone
Drug Central 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 None
100 3805 3H-QNB 58 Human Binding pKi = 6.0 6.0 -14 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 3H-QNB 58 Human Binding pKi = 6.0 6.0 -14 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 3H-QNB 58 Human Binding pKi = 6.0 6.0 -14 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 3H-QNB 58 Human Binding pKi = 6.0 6.0 -14 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 3H-QNB 58 Human Binding pKi = 6.0 6.0 -14 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
308 2060 3H-NMS 23 Rat Binding pKi = 7.0 7.0 -4 9
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
3603 2060 3H-NMS 23 Rat Binding pKi = 7.0 7.0 -4 9
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
CHEMBL1256682 2060 3H-NMS 23 Rat Binding pKi = 7.0 7.0 -4 9
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
2774 3868 3H-QNB 95 Rat Binding pKi = 7.0 7.0 -7 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 3868 3H-QNB 95 Rat Binding pKi = 7.0 7.0 -7 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593.0 3868 3H-QNB 95 Rat Binding pKi = 7.0 7.0 -7 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 3868 3H-QNB 95 Rat Binding pKi = 7.0 7.0 -7 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 3868 3H-QNB 95 Rat Binding pKi = 7.0 7.0 -7 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 3868 3H-QNB 95 Rat Binding pKi = 7.0 7.0 -7 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 3868 3H-QNB 95 Rat Binding pKi = 7.0 7.0 -7 9
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
135398745 2914 3H-QNB 112 Human Binding pKi = 6 6.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-QNB 112 Human Binding pKi = 6 6.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-QNB 112 Human Binding pKi = 6 6.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-QNB 112 Human Binding pKi = 6 6.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-QNB 112 Human Binding pKi = 6 6.0 -32 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
10104 3566 None 12 Human Binding pKi = 6.5 6.5 -9 6
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 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 3566 None 12 Human Binding pKi = 6.5 6.5 -9 6
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 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 3566 None 12 Human Binding pKi = 6.5 6.5 -9 6
Binding to hM4 receptors expressed in CHO cells.Binding to hM4 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 3322 None 0 Human Binding pKi = 9.3 9.3 -1 5
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</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>4</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 3322 None 0 Human Binding pKi = 9.3 9.3 -1 5
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</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>4</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
11753673.0 3322 None 0 Human Binding pKi = 9.3 9.3 -1 5
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</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>4</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 3322 None 0 Human Binding pKi = 9.3 9.3 -1 5
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</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>4</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 3322 None 0 Human Binding pKi = 9.3 9.3 -1 5
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</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>4</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 3322 None 0 Human Binding pKi = 9.3 9.3 -1 5
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>4</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>4</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 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
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 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
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
2684.0 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
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
584 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
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 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
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 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
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
DB00185 883 None 29 Human Binding pKi = 6.0 6.0 -1 4
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
11434515 261 None 6 Human Binding pKi = 10 10.0 1 5
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
11434515.0 261 None 6 Human Binding pKi = 10 10.0 1 5
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 261 None 6 Human Binding pKi = 10 10.0 1 5
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 261 None 6 Human Binding pKi = 10 10.0 1 5
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 261 None 6 Human Binding pKi = 10 10.0 1 5
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 261 None 6 Human Binding pKi = 10 10.0 1 5
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 261 None 6 Human Binding pKi = 10 10.0 1 5
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
2293 3186 None 27 Human Binding pKi = 10.2 10.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
329 3186 None 27 Human Binding pKi = 10.2 10.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
4934 3186 None 27 Human Binding pKi = 10.2 10.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
4934.0 3186 None 27 Human Binding pKi = 10.2 10.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
CHEMBL1180725 3186 None 27 Human Binding pKi = 10.2 10.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
DB00782 3186 None 27 Human Binding pKi = 10.2 10.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
11519069 3939 None 3 Human Binding pKi = 10.3 10.3 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
11519070 3939 None 3 Human Binding pKi = 10.3 10.3 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
11519070.0 3939 None 3 Human Binding pKi = 10.3 10.3 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
4816 3939 None 3 Human Binding pKi = 10.3 10.3 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
7354 3939 None 3 Human Binding pKi = 10.3 10.3 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
CHEMBL1187833 3939 None 3 Human Binding pKi = 10.3 10.3 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
DB09076 3939 None 3 Human Binding pKi = 10.3 10.3 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
367 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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
5487427.0 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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
5487427.0 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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 3824 None 12 Human Binding pKi = 10.4 10.4 -10 8
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
23056 112 None 29 Human Binding pKi = 10.4 10.4 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 29860464
318 112 None 29 Human Binding pKi = 10.4 10.4 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 29860464
3260 112 None 29 Human Binding pKi = 10.4 10.4 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 29860464
CHEMBL12980 112 None 29 Human Binding pKi = 10.4 10.4 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 29860464
2370 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
2370 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
2370.0 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
2370.0 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
297 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
297 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
358 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
358 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
CHEMBL1482 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
CHEMBL1482 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
DB01019 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
DB01019 623 None 31 Human Binding pKi = 4 4.0 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
2551 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
2551 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
2551.0 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
2551.0 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
298 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
298 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
488 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
488 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
CHEMBL965 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
CHEMBL965 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
DB00411 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
DB00411 794 None 23 Human Binding pKi = 4.6 4.6 -21 11
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
187 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
187 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
187.0 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
187.0 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
294 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
294 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
65 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
65 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
8593 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
8593 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
CHEMBL667 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
CHEMBL667 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
DB03128 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
DB03128 255 None 39 Human Binding pKi = 5.1 5.1 -6 9
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
302 2977 None 25 Human Binding pKi = 5.2 5.2 -7 8
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
302 2977 None 25 Human Binding pKi = 5.2 5.2 -7 8
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
4630 2977 None 25 Human Binding pKi = 5.2 5.2 -7 8
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
4630 2977 None 25 Human Binding pKi = 5.2 5.2 -7 8
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
CHEMBL7634 2977 None 25 Human Binding pKi = 5.2 5.2 -7 8
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
CHEMBL7634 2977 None 25 Human Binding pKi = 5.2 5.2 -7 8
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
2166 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
2166 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
305 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
305 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
5910 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
5910 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
5910.0 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
5910.0 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
CHEMBL550 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
CHEMBL550 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
DB01085 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
DB01085 3123 None 49 Human Binding pKi = 5.2 5.2 -17 8
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
2230 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
2230 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
2230 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
296 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
296 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
296 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
CHEMBL7303 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
CHEMBL7303 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
CHEMBL7303 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
DB04365 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
DB04365 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
DB04365 465 None 60 Human Binding pKi = 5.5 5.5 -218 10
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
1726 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1726 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
1993 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1993 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
1993.0 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1993.0 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
7438 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
7438 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
CHEMBL978 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
CHEMBL978 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
DB06709 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
DB06709 2497 None 13 Rat Binding pKi = 5.8 5.8 -32 5
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
24768606 4030 None 58 Human Binding pKi = 5.9 5.9 -79 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
3274 4030 None 58 Human Binding pKi = 5.9 5.9 -79 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
CHEMBL1628667 4030 None 58 Human Binding pKi = 5.9 5.9 -79 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
129786 1891 None 0 Rat Binding pKi = 6.2 6.2 -17 4
UnclassifiedUnclassified
Guide to Pharmacology 379 2 3 5 0.8 NC(=N)N1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 8813552
3276 1891 None 0 Rat Binding pKi = 6.2 6.2 -17 4
UnclassifiedUnclassified
Guide to Pharmacology 379 2 3 5 0.8 NC(=N)N1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 8813552
154059 3637 None 51 Human Binding pKi = 6.8 6.8 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
154059.0 3637 None 51 Human Binding pKi = 6.8 6.8 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
2457 3637 None 51 Human Binding pKi = 6.8 6.8 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
7483 3637 None 51 Human Binding pKi = 6.8 6.8 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
CHEMBL1734 3637 None 51 Human Binding pKi = 6.8 6.8 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
DB01591 3637 None 51 Human Binding pKi = 6.8 6.8 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
2774 3868 None 95 Human Binding pKi = 6.9 6.9 1 9
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
5593 3868 None 95 Human Binding pKi = 6.9 6.9 1 9
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
5593.0 3868 None 95 Human Binding pKi = 6.9 6.9 1 9
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
7319 3868 None 95 Human Binding pKi = 6.9 6.9 1 9
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
CHEMBL1200604 3868 None 95 Human Binding pKi = 6.9 6.9 1 9
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
DB00809 3868 None 95 Human Binding pKi = 6.9 6.9 1 9
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
DB01199 3868 None 95 Human Binding pKi = 6.9 6.9 1 9
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 29860464
154734599 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
154734599 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
154734599 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
154734599 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
327 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
327 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
327 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
327 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
4108 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
4108 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
4108 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
4108 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
CHEMBL27673 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
CHEMBL27673 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
CHEMBL27673 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
CHEMBL27673 2503 None 12 Human Binding pKi = 7.1 7.1 -2 11
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
5282426 1466 None 0 Human Binding pKi = 7.2 7.2 -15 6
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
5282426.0 1466 None 0 Human Binding pKi = 7.2 7.2 -15 6
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
7549 1466 None 0 Human Binding pKi = 7.2 7.2 -15 6
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
CHEMBL108947 1466 None 0 Human Binding pKi = 7.2 7.2 -15 6
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
CHEMBL1492500 1466 None 0 Human Binding pKi = 7.2 7.2 -15 6
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
DB09167 1466 None 0 Human Binding pKi = 7.2 7.2 -15 6
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
2200 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
2200 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
2200 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
2200 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
2200 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
328 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
328 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
328 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
328 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
328 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
4848 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
4848 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
4848 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
4848 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
4848 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
4848.0 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
4848.0 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
4848.0 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
4848.0 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
4848.0 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
CHEMBL9967 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
CHEMBL9967 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
CHEMBL9967 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
CHEMBL9967 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
CHEMBL9967 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
DB00670 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
DB00670 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
DB00670 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
DB00670 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
DB00670 3131 None 46 Human Binding pKi = 7.3 7.3 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
11498 3019 None 41 Human Binding pKi = 7.5 7.5 38 6
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10576595
11498 3019 None 41 Human Binding pKi = 7.5 7.5 38 6
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 27085897
4995951 3019 None 41 Human Binding pKi = 7.5 7.5 38 6
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10576595
4995951 3019 None 41 Human Binding pKi = 7.5 7.5 38 6
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 27085897
CHEMBL59898 3019 None 41 Human Binding pKi = 7.5 7.5 38 6
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10576595
CHEMBL59898 3019 None 41 Human Binding pKi = 7.5 7.5 38 6
UnclassifiedUnclassified
Guide to Pharmacology 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 27085897
3652 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
3652 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
3652 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
3652 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
57 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
57 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
57 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
57 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
60809 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
60809 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
60809 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809.0 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
60809.0 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
60809.0 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
60809.0 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
CHEMBL21536 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
CHEMBL21536 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
CHEMBL21536 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
CHEMBL21536 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
DB15357 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
DB15357 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 35380782
DB15357 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
DB15357 4097 None 79 Human Binding pKi = 7.6 7.6 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
119357 304 None 49 Human Binding pKi = 7.7 7.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
119357 304 None 49 Human Binding pKi = 7.7 7.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 27085897
3264 304 None 49 Human Binding pKi = 7.7 7.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
3264 304 None 49 Human Binding pKi = 7.7 7.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 27085897
368 304 None 49 Human Binding pKi = 7.7 7.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
368 304 None 49 Human Binding pKi = 7.7 7.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 27085897
CHEMBL279453 304 None 49 Human Binding pKi = 7.7 7.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
CHEMBL279453 304 None 49 Human Binding pKi = 7.7 7.7 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 27085897
319 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
319 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
319 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
321 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
321 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
321 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
444031 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
444031 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
444031 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
444031.0 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
444031.0 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
444031.0 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
784 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
784 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
784 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
CHEMBL1346 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
CHEMBL1346 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
CHEMBL1346 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
DB00496 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
DB00496 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
DB00496 1324 None 44 Human Binding pKi = 7.7 7.7 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
132947 3864 None 9 Human Binding pKi = 7.9 7.9 -22 9
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 3864 None 9 Human Binding pKi = 7.9 7.9 -22 9
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 3864 None 9 Human Binding pKi = 7.9 7.9 -22 9
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
129989 451 None 51 Human Binding pKi = 8 8.0 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
129989 451 None 51 Human Binding pKi = 8 8.0 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
8584 451 None 51 Human Binding pKi = 8 8.0 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
8584 451 None 51 Human Binding pKi = 8 8.0 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
CHEMBL43383 451 None 51 Human Binding pKi = 8 8.0 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
CHEMBL43383 451 None 51 Human Binding pKi = 8 8.0 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
324 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
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 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
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 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
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 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
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 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
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 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
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 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
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 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
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 1925 None 15 Human Binding pKi = 8.1 8.1 -1 9
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
2200 3131 None 46 Human Binding pKi = 8.1 8.1 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
328 3131 None 46 Human Binding pKi = 8.1 8.1 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
4848 3131 None 46 Human Binding pKi = 8.1 8.1 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
4848.0 3131 None 46 Human Binding pKi = 8.1 8.1 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
CHEMBL9967 3131 None 46 Human Binding pKi = 8.1 8.1 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
DB00670 3131 None 46 Human Binding pKi = 8.1 8.1 -2 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 29860464
180 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
200 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
2160 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
2160.0 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
CHEMBL629 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
DB00321 401 None 56 Human Binding pKi = 8.1 8.1 -6 40
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
10894911 3018 None 0 Human Binding pKi = 8.2 8.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 412 6 1 4 5.3 c1ccc(cc1)CN1CCC(CC1)CCNc1nnc2c(c1)CCCc1c2cccc1 27085897
11499 3018 None 0 Human Binding pKi = 8.2 8.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 412 6 1 4 5.3 c1ccc(cc1)CN1CCC(CC1)CCNc1nnc2c(c1)CCCc1c2cccc1 27085897
CHEMBL88223 3018 None 0 Human Binding pKi = 8.2 8.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 412 6 1 4 5.3 c1ccc(cc1)CN1CCC(CC1)CCNc1nnc2c(c1)CCCc1c2cccc1 27085897
3042 1414 None 35 Human Binding pKi = 8.3 8.3 -1 14
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
3042.0 1414 None 35 Human Binding pKi = 8.3 8.3 -1 14
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
355 1414 None 35 Human Binding pKi = 8.3 8.3 -1 14
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
868 1414 None 35 Human Binding pKi = 8.3 8.3 -1 14
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
CHEMBL1123 1414 None 35 Human Binding pKi = 8.3 8.3 -1 14
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
DB00804 1414 None 35 Human Binding pKi = 8.3 8.3 -1 14
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 29860464
2705 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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
443879.0 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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
443879.0 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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 3842 None 64 Human Binding pKi = 8.4 8.4 -1 10
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
129140 3934 None 0 Human Binding pKi = 8.4 8.4 1 4
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 2043926
129140 3934 None 0 Human Binding pKi = 8.4 8.4 1 4
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 9671109
8583 3934 None 0 Human Binding pKi = 8.4 8.4 1 4
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 2043926
8583 3934 None 0 Human Binding pKi = 8.4 8.4 1 4
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 9671109
324 1925 None 15 Human Binding pKi = 8.4 8.4 -1 9
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 29860464
6436265 1925 None 15 Human Binding pKi = 8.4 8.4 -1 9
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 29860464
CHEMBL277642 1925 None 15 Human Binding pKi = 8.4 8.4 -1 9
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 29860464
313 2691 None 0 Human Binding pKi = 8.5 8.5 2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 29860464
2028 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
2028 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
359 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
359 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
4634 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
4634 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
4634.0 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
4634.0 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
CHEMBL1231 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
CHEMBL1231 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
DB01062 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
DB01062 2979 None 80 Human Binding pKi = 8.6 8.6 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
313 2691 None 0 Human Binding pKi = 8.7 8.7 2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7925952
313 2691 None 0 Human Binding pKi = 8.7 8.7 2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9862767
1734 116 None 10 Human Binding pKi = 8.9 8.9 -1 12
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
307 116 None 10 Human Binding pKi = 8.9 8.9 -1 12
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
CHEMBL168067 116 None 10 Human Binding pKi = 8.9 8.9 -1 12
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
174174 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
174174.0 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
174174.0 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
174174.0 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
174174.0 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
260 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
260 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
260 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
260 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
320 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
320 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
320 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
320 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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 523 None 49 Human Binding pKi = 9.1 9.1 -2 14
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
325 2062 None 0 Human Binding pKi = 9.2 9.2 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
3746 2062 None 0 Human Binding pKi = 9.2 9.2 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
657308 2062 None 0 Human Binding pKi = 9.2 9.2 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
CHEMBL1615433 2062 None 0 Human Binding pKi = 9.2 9.2 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
DB00332 2062 None 0 Human Binding pKi = 9.2 9.2 -1 8
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
3000322 3562 None 38 Human Binding pKi = 9.3 9.3 -1 6
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 3562 None 38 Human Binding pKi = 9.3 9.3 -1 6
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
3000322.0 3562 None 38 Human Binding pKi = 9.3 9.3 -1 6
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
3000322.0 3562 None 38 Human Binding pKi = 9.3 9.3 -1 6
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 3562 None 38 Human Binding pKi = 9.3 9.3 -1 6
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 3562 None 38 Human Binding pKi = 9.3 9.3 -1 6
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 3562 None 38 Human Binding pKi = 9.3 9.3 -1 6
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 3562 None 38 Human Binding pKi = 9.3 9.3 -1 6
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 3562 None 38 Human Binding pKi = 9.3 9.3 -1 6
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 3562 None 38 Human Binding pKi = 9.3 9.3 -1 6
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
10470 2488 None 7 Human Binding pKi = 9.4 9.4 4 3
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
1689 2488 None 7 Human Binding pKi = 9.4 9.4 4 3
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
4057 2488 None 7 Human Binding pKi = 9.4 9.4 4 3
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
4057.0 2488 None 7 Human Binding pKi = 9.4 9.4 4 3
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
CHEMBL524004 2488 None 7 Human Binding pKi = 9.4 9.4 4 3
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
DB04843 2488 None 7 Human Binding pKi = 9.4 9.4 4 3
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 29860464
8586 301 None 0 Human Binding pKi = 9.5 9.5 -2 4
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 301 None 0 Human Binding pKi = 9.5 9.5 -2 4
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
11693 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
11693 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
3494 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
3494 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
3494.0 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
3494.0 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
4302 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
4302 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
7459 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
7459 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
9933193.0 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
9933193.0 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
CHEMBL1201335 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
CHEMBL1201335 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
DB00986 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
DB00986 1827 None 16 Human Binding pKi = 9.6 9.6 1 5
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
174174 523 None 49 Rat Binding pKi = 9.7 9.7 1 14
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
174174.0 523 None 49 Rat Binding pKi = 9.7 9.7 1 14
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
260 523 None 49 Rat Binding pKi = 9.7 9.7 1 14
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
320 523 None 49 Rat Binding pKi = 9.7 9.7 1 14
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 523 None 49 Rat Binding pKi = 9.7 9.7 1 14
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 523 None 49 Rat Binding pKi = 9.7 9.7 1 14
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
2039 2982 None 19 Human Binding pKi = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
5749 2982 None 19 Human Binding pKi = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
5749.0 2982 None 19 Human Binding pKi = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
7257 2982 None 19 Human Binding pKi = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
CHEMBL1201286 2982 None 19 Human Binding pKi = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
DB00219 2982 None 19 Human Binding pKi = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 29860464
314 2692 None 0 Human Binding pKi > 5 5.0 -1122018 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10799315
3337 206367 None 27 Human Binding pKi None 8.3 8.3 -190 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337.0 206367 None 27 Human Binding pKi None 8.3 8.3 -190 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 None 27 Human Binding pKi None 8.3 8.3 -190 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 None 27 Human Binding pKi None 8.3 8.3 -190 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 None 27 Human Binding pKi None 8.3 8.3 -190 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 None 27 Human Binding pKi None 8.3 8.3 -190 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206367 None 27 Human Binding pKi None 8.3 8.3 -190 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
2865 4143 None 73 Human Binding pKi None 8.2 8.2 -912 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 None 73 Human Binding pKi None 8.2 8.2 -912 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 None 73 Human Binding pKi None 8.2 8.2 -912 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854.0 4143 None 73 Human Binding pKi None 8.2 8.2 -912 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 None 73 Human Binding pKi None 8.2 8.2 -912 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 None 73 Human Binding pKi None 8.2 8.2 -912 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
3012003 216145 None 0 Human Binding pKi None 8.2 8.2 -2 12
NoneNone
Drug Central 311 5 0 3 3.8 CN1CCC(C(C1)COC2=CC=C(C=C2)OC)C3=CC=CC=C3 None
11976 920 None 59 Human Binding pKi None 8.1 8.1 -11 24
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 None 59 Human Binding pKi None 8.1 8.1 -11 24
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467.0 920 None 59 Human Binding pKi None 8.1 8.1 -11 24
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 None 59 Human Binding pKi None 8.1 8.1 -11 24
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 None 59 Human Binding pKi None 8.1 8.1 -11 24
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
4066 204626 None 78 Human Binding pKi None 8.1 8.1 -1 7
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
4066.0 204626 None 78 Human Binding pKi None 8.1 8.1 -1 7
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
CHEMBL73451 204626 None 78 Human Binding pKi None 8.1 8.1 -1 7
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
DB01071 204626 None 78 Human Binding pKi None 8.1 8.1 -1 7
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
10938 1702 None 0 Human Binding pKi None 4.3 4.3 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
299 1702 None 0 Human Binding pKi None 4.3 4.3 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
3256 1702 None 0 Human Binding pKi None 4.3 4.3 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
CHEMBL2110739 1702 None 0 Human Binding pKi None 4.3 4.3 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
300 2510 None 15 Human Binding pKi None 4.7 4.7 -3 6
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
4141 2510 None 15 Human Binding pKi None 4.7 4.7 -3 6
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
CHEMBL92387 2510 None 15 Human Binding pKi None 4.7 4.7 -3 6
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
303 2978 None 17 Human Binding pKi None 5.2 5.2 -70 6
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
4629 2978 None 17 Human Binding pKi None 5.2 5.2 -70 6
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
8595 2978 None 17 Human Binding pKi None 5.2 5.2 -70 6
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
CHEMBL44674 2978 None 17 Human Binding pKi None 5.2 5.2 -70 6
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
22991950 2328 None 0 Human Binding pKi None 5.3 5.3 -5 6
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 2328 None 0 Human Binding pKi None 5.3 5.3 -5 6
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
301 2534 None 19 Human Binding pKi None 5.5 5.5 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
9571002 2534 None 19 Human Binding pKi None 5.5 5.5 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
CHEMBL151938 2534 None 19 Human Binding pKi None 5.5 5.5 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
2229 464 None 22 Human Binding pKi None 5.9 5.9 -2 6
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
295 464 None 22 Human Binding pKi None 5.9 5.9 -2 6
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
CHEMBL128365 464 None 22 Human Binding pKi None 5.9 5.9 -2 6
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
312 2690 None 0 Human Binding pKi None 5.9 5.9 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12512959
290 2473 None 6 Human Binding pKi None 6.2 6.2 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7680092
4022 2473 None 6 Human Binding pKi None 6.2 6.2 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7680092
5926 2473 None 6 Human Binding pKi None 6.2 6.2 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7680092
CHEMBL40554 2473 None 6 Human Binding pKi None 6.2 6.2 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7680092
CHEMBL74300 2473 None 6 Human Binding pKi None 6.2 6.2 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7680092
107867 2974 None 55 Rat Binding pKi None 6.5 6.5 -4 11
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
309 2974 None 55 Rat Binding pKi None 6.5 6.5 -4 11
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
CHEMBL17045 2974 None 55 Rat Binding pKi None 6.5 6.5 -4 11
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
310 1922 None 0 Human Binding pKi None 7.1 7.1 -4 10
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
310 1922 None 0 Human Binding pKi None 7.1 7.1 -4 10
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
3602 1922 None 0 Human Binding pKi None 7.1 7.1 -4 10
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
3602 1922 None 0 Human Binding pKi None 7.1 7.1 -4 10
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
CHEMBL3545990 1922 None 0 Human Binding pKi None 7.1 7.1 -4 10
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
CHEMBL3545990 1922 None 0 Human Binding pKi None 7.1 7.1 -4 10
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
124226 1921 None 0 Human Binding pKi None 7.1 7.1 -7 5
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
322 1921 None 0 Human Binding pKi None 7.1 7.1 -7 5
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
311 2689 None 0 Human Binding pKi None 7.1 7.1 -2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12512959
2200 3131 None 46 Rat Binding pKi None 7.1 7.1 -7 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
328 3131 None 46 Rat Binding pKi None 7.1 7.1 -7 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
4848 3131 None 46 Rat Binding pKi None 7.1 7.1 -7 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
4848.0 3131 None 46 Rat Binding pKi None 7.1 7.1 -7 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
CHEMBL9967 3131 None 46 Rat Binding pKi None 7.1 7.1 -7 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
DB00670 3131 None 46 Rat Binding pKi None 7.1 7.1 -7 12
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
306 3456 None 21 Human Binding pKi None 7.2 7.2 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
3536 3456 None 21 Human Binding pKi None 7.2 7.2 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
53930639 3456 None 21 Human Binding pKi None 7.2 7.2 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
9577995 3456 None 21 Human Binding pKi None 7.2 7.2 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
CHEMBL134641 3456 None 21 Human Binding pKi None 7.2 7.2 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
308 2060 None 23 Human Binding pKi None 7.3 7.3 -2 9
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
308 2060 None 23 Human Binding pKi None 7.3 7.3 -2 9
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
3603 2060 None 23 Human Binding pKi None 7.3 7.3 -2 9
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
3603 2060 None 23 Human Binding pKi None 7.3 7.3 -2 9
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
CHEMBL1256682 2060 None 23 Human Binding pKi None 7.3 7.3 -2 9
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
CHEMBL1256682 2060 None 23 Human Binding pKi None 7.3 7.3 -2 9
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
10426487 2841 None 7 Human Binding pKi None 7.3 7.3 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
291 2841 None 7 Human Binding pKi None 7.3 7.3 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
CHEMBL99521 2841 None 7 Human Binding pKi None 7.3 7.3 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
310 1922 None 0 Rat Binding pKi None 7.7 7.7 -10 10
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 1325587
3602 1922 None 0 Rat Binding pKi None 7.7 7.7 -10 10
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 1325587
CHEMBL3545990 1922 None 0 Rat Binding pKi None 7.7 7.7 -10 10
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 1325587
293 2843 None 0 Human Binding pKi None 8.1 8.1 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1cccc(c1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
9985526 2843 None 0 Human Binding pKi None 8.1 8.1 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1cccc(c1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
1371 1923 None 11 Human Binding pKi None 8.3 8.3 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
24199 1923 None 11 Human Binding pKi None 8.3 8.3 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
24199.0 1923 None 11 Human Binding pKi None 8.3 8.3 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
323 1923 None 11 Human Binding pKi None 8.3 8.3 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
CHEMBL1201325 1923 None 11 Human Binding pKi None 8.3 8.3 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
DB06787 1923 None 11 Human Binding pKi None 8.3 8.3 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
130169 3605 None 0 Human Binding pKi None 8.5 8.5 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O 2704370
331 3605 None 0 Human Binding pKi None 8.5 8.5 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O 2704370
11757797 2842 None 0 Human Binding pKi None 8.6 8.6 -31 5
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccc(cc1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
292 2842 None 0 Human Binding pKi None 8.6 8.6 -31 5
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccc(cc1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
10062394 3047 None 1 Human Binding pKi None 8.7 8.7 1 4
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
304 3047 None 1 Human Binding pKi None 8.7 8.7 1 4
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
CHEMBL130715 3047 None 1 Human Binding pKi None 8.7 8.7 1 4
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
1734 116 None 10 Rat Binding pKi None 9.1 9.1 -3 12
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587
307 116 None 10 Rat Binding pKi None 9.1 9.1 -3 12
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587
CHEMBL168067 116 None 10 Rat Binding pKi None 9.1 9.1 -3 12
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587