Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL143434 acm4_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
565 15 0 10 6.3 CN1CCC=C(C1)C2=NSN=C2SCCCCCCCCCCSC3=NSN=C3C4=CCCN(C4)C
CHEMBL139603 acm4_human Human No 9.0 EC50 = 1 Funct
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
593 17 0 10 7.4 CN1CCC=C(C1)C2=NSN=C2SCCCCCCCCCCCCSC3=NSN=C3C4=CCCN(C4)C
CHEMBL142538 acm4_human Human No 8.9 EC50 = 1.4 Funct
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
561 17 0 10 6.3 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCCCCOC3=NSN=C3C4=CCCN(C4)C
CHEMBL1223860 acm4_human Human No 7.0 EC50 = 100 Funct
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
390 4 0 5 4.1 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=C(C(=C4)C)F)OC3=O
CHEMBL1223860 acm4_human Human No 7.0 EC50 = 100 Funct
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
390 4 0 5 4.1 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=C(C(=C4)C)F)OC3=O
CHEMBL2313395 acm4_human Human No 7.0 EC50 = 104 Funct
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
360 3 2 4 4.9 CC1=CC=C(C=C1)CNC(=O)C2=C(C3=C(C(=C(N=C3S2)C)Cl)C)N
CHEMBL3810071 acm4_human Human No 6.0 EC50 = 1047.1 Funct
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
337 3 0 5 3.2 CC1=C2C(=NC(=NN2C=C1)C)N3CCC(CC3)OC4=CN=C(C=C4)C
CHEMBL3810071 acm4_human Human No 6.0 EC50 = 1047.1 Funct
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
337 3 0 5 3.2 CC1=C2C(=NC(=NN2C=C1)C)N3CCC(CC3)OC4=CN=C(C=C4)C
CHEMBL3616501 acm4_human Human Yes 6.0 EC50 = 1060 Funct
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
508 7 2 4 5.0 CC(=NC1=CC2=C(CC(C2NC(=O)C3=CC=C(C=C3)C4=CC=CC=C4)O)C=C1)N(C)CC5=CC=C(C=C5)F
CHEMBL3616501 acm4_human Human Yes 6.0 EC50 = 1060 Funct
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
508 7 2 4 5.0 CC(=NC1=CC2=C(CC(C2NC(=O)C3=CC=C(C=C3)C4=CC=CC=C4)O)C=C1)N(C)CC5=CC=C(C=C5)F
CHEMBL2313375 acm4_human Human No 7.0 EC50 = 107 Funct
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
376 4 2 5 4.5 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CC=C(C=C3)OC)N
CHEMBL2313392 acm4_human Human No 7.0 EC50 = 108 Funct
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
346 3 2 4 4.6 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CC=CC=C3)N
CHEMBL3810071 acm4_human Human No 6.0 EC50 = 1100 Funct
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
337 3 0 5 3.2 CC1=C2C(=NC(=NN2C=C1)C)N3CCC(CC3)OC4=CN=C(C=C4)C
CHEMBL3809603 acm4_human Human Yes 6.0 EC50 = 1100 Funct
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
344 2 0 5 3.2 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCCC4)C
CHEMBL143468 acm4_human Human No 6.0 EC50 = 1100 Funct
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
533 15 0 10 5.2 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCCOC3=NSN=C3C4=CCCN(C4)C
CHEMBL3618436 acm4_human Human No 6.0 EC50 = 1110 Funct
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
482 5 3 4 4.0 CC(=NC1=CC=C(C=C1)F)NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL3618436 acm4_human Human No 6.0 EC50 = 1110 Funct
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
482 5 3 4 4.0 CC(=NC1=CC=C(C=C1)F)NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL2057394 acm4_human Human Yes 6.0 EC50 = 1122.0 Funct
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
300 3 1 6 2.1 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=NC=CN=C3
CHEMBL2057394 acm4_human Human Yes 6.0 EC50 = 1122.0 Funct
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
300 3 1 6 2.1 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=NC=CN=C3
CHEMBL3616504 acm4_human Human No 7.0 EC50 = 113 Funct
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
442 3 2 3 2.9 CN1CCCCC1=NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL3616504 acm4_human Human No 7.0 EC50 = 113 Funct
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
442 3 2 3 2.9 CN1CCCCC1=NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL3809603 acm4_human Human Yes 5.9 EC50 = 1148.2 Funct
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
344 2 0 5 3.2 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCCC4)C
CHEMBL3809603 acm4_human Human Yes 5.9 EC50 = 1148.2 Funct
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
344 2 0 5 3.2 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCCC4)C
CHEMBL3618440 acm4_human Human No 6.9 EC50 = 115 Funct
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
496 6 3 4 3.9 CC(=NCC1=CC=C(C=C1)F)NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL3618440 acm4_human Human No 6.9 EC50 = 115 Funct
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
496 6 3 4 3.9 CC(=NCC1=CC=C(C=C1)F)NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL3809292 acm4_human Human No 5.9 EC50 = 1174.9 Funct
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
334 3 0 5 3.9 CC1=CC2=C(C=C1)N=CN=C2N3CCC(CC3)OC4=CN=C(C=C4)C
CHEMBL3809292 acm4_human Human No 5.9 EC50 = 1174.9 Funct
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
334 3 0 5 3.9 CC1=CC2=C(C=C1)N=CN=C2N3CCC(CC3)OC4=CN=C(C=C4)C
CHEMBL1223754 acm4_human Human No 7.9 EC50 = 12.6 Funct
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
404 5 1 4 4.1 CCCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=C(C(=C4)C)F)NC3=O
CHEMBL1223754 acm4_human Human No 7.9 EC50 = 12.6 Funct
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
404 5 1 4 4.1 CCCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=C(C(=C4)C)F)NC3=O
CHEMBL3809292 acm4_human Human No 5.9 EC50 = 1200 Funct
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
334 3 0 5 3.9 CC1=CC2=C(C=C1)N=CN=C2N3CCC(CC3)OC4=CN=C(C=C4)C
CHEMBL1357034 acm4_human Human Yes 5.9 EC50 = 1202.3 Funct
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
446 4 2 8 2.7 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)S(=O)(=O)N)C
CHEMBL1357034 acm4_human Human Yes 5.9 EC50 = 1202.3 Funct
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
446 4 2 8 2.7 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)S(=O)(=O)N)C
CHEMBL2313376 acm4_human Human No 6.9 EC50 = 124 Funct
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
382 3 2 6 4.8 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=C(C(=CC=C3)F)F)N
CHEMBL1223807 acm4_human Human No 6.9 EC50 = 125.9 Funct
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
358 4 0 4 3.7 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=CC=CC=C4OC3=O
CHEMBL1223807 acm4_human Human No 6.9 EC50 = 125.9 Funct
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
358 4 0 4 3.7 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=CC=CC=C4OC3=O
CHEMBL2313384 acm4_human Human No 6.9 EC50 = 128 Funct
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
361 4 2 5 4.0 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCCC3=CC=NC=C3)N
CHEMBL2057392 acm4_human Human Yes 5.9 EC50 = 1288.3 Funct
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
299 3 1 5 2.8 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=CC=NC=C3
CHEMBL2057392 acm4_human Human Yes 5.9 EC50 = 1288.3 Funct
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
299 3 1 5 2.8 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=CC=NC=C3
CHEMBL3289442 acm4_human Human No 7.9 EC50 = 13 Funct
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
451 5 0 7 2.1 CCOC(=O)N1CCC(CC1)(C)CN2CCC3(CC2)CN(C4=C3C=CC=N4)S(=O)(=O)C
CHEMBL3289442 acm4_human Human No 7.9 EC50 = 13 Funct
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
451 5 0 7 2.1 CCOC(=O)N1CCC(CC1)(C)CN2CCC3(CC2)CN(C4=C3C=CC=N4)S(=O)(=O)C
CHEMBL7303 acm4_human Human Yes 6.9 EC50 = 130 Funct
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)
155 2 0 3 0.3 CN1CCC=C(C1)C(=O)OC
CHEMBL1212983 acm4_rat Rat Yes 5.9 EC50 = 1300 Funct
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
311 3 2 4 3.9 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=CC=C3)N)C
CHEMBL1212983 acm4_rat Rat Yes 5.9 EC50 = 1300 Funct
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
311 3 2 4 3.9 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=CC=C3)N)C
CHEMBL2057376 acm4_human Human Yes 5.9 EC50 = 1349.0 Funct
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
288 3 1 5 3.3 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=CC=CO3
CHEMBL2057376 acm4_human Human Yes 5.9 EC50 = 1349.0 Funct
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
288 3 1 5 3.3 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=CC=CO3
CHEMBL3616497 acm4_human Human No 5.9 EC50 = 1360 Funct
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
522 8 3 4 4.1 CC(=NCCC1=CC=C(C=C1)OC)NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL3616497 acm4_human Human No 5.9 EC50 = 1360 Funct
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
522 8 3 4 4.1 CC(=NCCC1=CC=C(C=C1)OC)NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL2313383 acm4_human Human No 5.9 EC50 = 1370 Funct
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
361 3 2 5 3.9 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC(C)C3=CC=CC=N3)N
CHEMBL2313374 acm4_human Human No 5.9 EC50 = 1410 Funct
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
352 3 2 4 5.4 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3CCCCC3)N
CHEMBL2313404 acm4_human Human No 6.8 EC50 = 147 Funct
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
298 2 2 4 3.9 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC(C)C)N
CHEMBL2313377 acm4_rat Rat No 6.8 EC50 = 147 Funct
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
296 2 2 4 3.6 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC3CC3)N
CHEMBL2336056 acm4_human Human No 7.8 EC50 = 15 Funct
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
386 5 0 4 2.6 CCOC(=O)N1CCC(CC1)(C)CN2CCC(C2)N3C(=O)CC4=CC=CC=C43
CHEMBL965 acm4_human Human Yes 6.8 EC50 = 154.9 Funct
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
147 4 1 2 -0.4 C[N+](C)(C)CCOC(=O)N
CHEMBL965 acm4_human Human Yes 6.8 EC50 = 154.9 Funct
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
147 4 1 2 -0.4 C[N+](C)(C)CCOC(=O)N
CHEMBL1223862 acm4_human Human No 6.8 EC50 = 158.5 Funct
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
389 5 0 5 3.6 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=CC(=C4)OC)OC3=O
CHEMBL1223805 acm4_human Human No 6.8 EC50 = 158.5 Funct
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
357 3 0 3 3.3 CC1=CC2=C(CC(=O)N2C3CCN(CC3)C4(CCC(CC4)OC)C)C=C1
CHEMBL1223862 acm4_human Human No 6.8 EC50 = 158.5 Funct
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
389 5 0 5 3.6 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=CC(=C4)OC)OC3=O
CHEMBL1223805 acm4_human Human No 6.8 EC50 = 158.5 Funct
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
357 3 0 3 3.3 CC1=CC2=C(CC(=O)N2C3CCN(CC3)C4(CCC(CC4)OC)C)C=C1
CHEMBL1223864 acm4_human Human No 5.8 EC50 = 1584.9 Funct
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
437 5 0 6 2.9 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=CC(=C4)S(=O)(=O)C)OC3=O
CHEMBL1223938 acm4_human Human No 5.8 EC50 = 1584.9 Funct
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
451 6 0 6 3.3 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=CC(=C4)S(=O)(=O)CC)OC3=O
CHEMBL1603219 acm4_human Human Yes 5.8 EC50 = 1584.9 Funct
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
419 3 1 6 4.8 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=C(C=C(C=C4)F)Cl)C
CHEMBL1223864 acm4_human Human No 5.8 EC50 = 1584.9 Funct
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
437 5 0 6 2.9 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=CC(=C4)S(=O)(=O)C)OC3=O
CHEMBL1223938 acm4_human Human No 5.8 EC50 = 1584.9 Funct
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
451 6 0 6 3.3 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=CC(=C4)S(=O)(=O)CC)OC3=O
CHEMBL1603219 acm4_human Human Yes 5.8 EC50 = 1584.9 Funct
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
419 3 1 6 4.8 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=C(C=C(C=C4)F)Cl)C
CHEMBL1357034 acm4_rat Rat Yes 6.8 EC50 = 160 Funct
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
446 4 2 8 2.7 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)S(=O)(=O)N)C
CHEMBL2313394 acm4_human Human Yes 6.8 EC50 = 160 Funct
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
380 3 2 4 5.2 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CC=CC=C3Cl)N
CHEMBL2313393 acm4_human Human No 6.8 EC50 = 160 Funct
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
382 3 2 6 4.8 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CC(=C(C=C3)F)F)N
CHEMBL1357034 acm4_rat Rat Yes 6.8 EC50 = 160 Funct
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
446 4 2 8 2.7 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)S(=O)(=O)N)C
CHEMBL1603219 acm4_human Human Yes 5.8 EC50 = 1600 Funct
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
419 3 1 6 4.8 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=C(C=C(C=C4)F)Cl)C
CHEMBL3808425 acm4_human Human Yes 5.8 EC50 = 1698.2 Funct
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
360 2 0 6 2.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCOCC4)C
CHEMBL3808425 acm4_human Human Yes 5.8 EC50 = 1698.2 Funct
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
360 2 0 6 2.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCOCC4)C
CHEMBL3808425 acm4_human Human Yes 5.8 EC50 = 1700 Funct
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
360 2 0 6 2.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCOCC4)C
CHEMBL3809693 acm4_human Human No 5.8 EC50 = 1737.8 Funct
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
358 3 0 7 4.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CN=C(C=C4)F)C
CHEMBL3809693 acm4_human Human No 5.8 EC50 = 1737.8 Funct
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
358 3 0 7 4.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CN=C(C=C4)F)C
CHEMBL2313398 acm4_human Human No 5.8 EC50 = 1750 Funct
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
414 3 2 7 5.5 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CC=C(C=C3)C(F)(F)F)N
CHEMBL2057417 acm4_rat Rat No 6.8 EC50 = 176 Funct
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
347 3 2 5 3.5 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CC=NC=C3)N
CHEMBL3354068 acm4_human Human No 7.7 EC50 = 18.6 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354068 acm4_human Human No 7.7 EC50 = 18.6 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL2313396 acm4_human Human Yes 6.8 EC50 = 180 Funct
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
380 3 2 4 5.2 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CC=C(C=C3)Cl)N
CHEMBL3809693 acm4_human Human No 5.8 EC50 = 1800 Funct
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
358 3 0 7 4.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CN=C(C=C4)F)C
CHEMBL1424504 acm4_human Human Yes 5.7 EC50 = 1819.7 Funct
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
306 3 1 6 2.4 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=COCCO3
CHEMBL1424504 acm4_human Human Yes 5.7 EC50 = 1819.7 Funct
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
306 3 1 6 2.4 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=COCCO3
CHEMBL1354105 acm4_rat Rat No 6.7 EC50 = 183.1 Funct
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)
440 6 2 8 4.5 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=C(C=CC(=C3)F)F)N)OCC4=CC=NC=C4
CHEMBL1354105 acm4_rat Rat No 6.7 EC50 = 183.1 Funct
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)
440 6 2 8 4.5 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=C(C=CC(=C3)F)F)N)OCC4=CC=NC=C4
CHEMBL3808696 acm4_human Human No 5.7 EC50 = 1862.1 Funct
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
394 2 0 7 3.9 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCCC(C4)(F)F)C
CHEMBL3808696 acm4_human Human No 5.7 EC50 = 1862.1 Funct
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
394 2 0 7 3.9 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCCC(C4)(F)F)C
CHEMBL3808696 acm4_human Human No 5.7 EC50 = 1900 Funct
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
394 2 0 7 3.9 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCCC(C4)(F)F)C
CHEMBL1593296 acm4_rat Rat No 6.7 EC50 = 191.6 Funct
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)
393 6 2 7 3.0 CC1=CC(=NC2=C1C(=C(S2)C(=O)NC(C)(C)C)N)OCCN3CCOCC3
CHEMBL1593296 acm4_rat Rat No 6.7 EC50 = 191.6 Funct
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)
393 6 2 7 3.0 CC1=CC(=NC2=C1C(=C(S2)C(=O)NC(C)(C)C)N)OCCN3CCOCC3
CHEMBL1223861 acm4_human Human No 6.7 EC50 = 199.5 Funct
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
390 4 0 5 4.1 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C(=CC(=C4)C)F)OC3=O
CHEMBL1223940 acm4_human Human No 6.7 EC50 = 199.5 Funct
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
403 6 0 5 3.5 CC1=CC2=C(C=C1)OC(=O)N2C3CCN(CC3)C4(CCC(CC4)OCCOC)C
CHEMBL2146598 acm4_human Human No 6.7 EC50 = 199.5 Funct
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
301 2 1 3 2.4 C1CN(CCC1N2C3=CC=CC=C3NC2=O)C4CCOCC4
CHEMBL1223861 acm4_human Human No 6.7 EC50 = 199.5 Funct
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
390 4 0 5 4.1 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C(=CC(=C4)C)F)OC3=O
CHEMBL1223940 acm4_human Human No 6.7 EC50 = 199.5 Funct
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
403 6 0 5 3.5 CC1=CC2=C(C=C1)OC(=O)N2C3CCN(CC3)C4(CCC(CC4)OCCOC)C
CHEMBL2146598 acm4_human Human No 6.7 EC50 = 199.5 Funct
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
301 2 1 3 2.4 C1CN(CCC1N2C3=CC=CC=C3NC2=O)C4CCOCC4
CHEMBL3354073 acm4_human Human No 5.7 EC50 = 1995.3 Funct
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
359 9 1 3 3.5 C1CN(CCC1CCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354073 acm4_human Human No 5.7 EC50 = 1995.3 Funct
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
359 9 1 3 3.5 C1CN(CCC1CCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL143469 acm4_human Human No 4.7 EC50 = 20000 Funct
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
519 14 0 10 4.7 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCOC3=NSN=C3C4=CCCN(C4)C
CHEMBL2313403 acm4_human Human No 5.7 EC50 = 2010 Funct
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
312 2 2 5 2.8 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC3COC3)N
CHEMBL2313380 acm4_human Human No 6.7 EC50 = 208 Funct
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
347 3 2 5 3.5 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CN=CC=C3)N
CHEMBL134641 acm4_human Human Yes 6.7 EC50 = 214 Funct
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
193 2 0 4 1.0 CON=C(C#N)C1CN2CCC1CC2
CHEMBL134641 acm4_human Human Yes 6.7 EC50 = 214 Funct
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
193 2 0 4 1.0 CON=C(C#N)C1CN2CCC1CC2
CHEMBL1978713 acm4_rat Rat Yes 6.7 EC50 = 225 Funct
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
341 4 2 5 3.9 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)OC)N)C
CHEMBL2057392 acm4_rat Rat Yes 6.7 EC50 = 225 Funct
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
299 3 1 5 2.8 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=CC=NC=C3
CHEMBL3808485 acm4_rat Rat No 6.7 EC50 = 225 Funct
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
338 3 0 6 3.6 CC1=NC=C(C=C1)OC2CCN(CC2)C3=NC=NC4=C3C=C(C=C4)F
CHEMBL2313073 acm4_human Human Yes 6.7 EC50 = 226 Funct
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
338 2 2 4 4.9 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC3CCCCC3)N
CHEMBL3618445 acm4_human Human No 6.6 EC50 = 227 Funct
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
496 6 3 4 3.9 CC(=NCC1=CC=CC=C1F)NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL3618445 acm4_human Human No 6.6 EC50 = 227 Funct
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
496 6 3 4 3.9 CC(=NCC1=CC=CC=C1F)NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL965 acm4_human Human Yes 5.6 EC50 = 2290.9 Funct
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
147 4 1 2 -0.4 C[N+](C)(C)CCOC(=O)N
CHEMBL3810300 acm4_human Human No 5.6 EC50 = 2290.9 Funct
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
381 3 0 6 5.0 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CC5=C(C=C4)OCC5)C
CHEMBL965 acm4_human Human Yes 5.6 EC50 = 2290.9 Funct
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
147 4 1 2 -0.4 C[N+](C)(C)CCOC(=O)N
CHEMBL3810300 acm4_human Human No 5.6 EC50 = 2290.9 Funct
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
381 3 0 6 5.0 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CC5=C(C=C4)OCC5)C
CHEMBL1978713 acm4_rat Rat Yes 6.6 EC50 = 230 Funct
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
341 4 2 5 3.9 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)OC)N)C
CHEMBL3809384 acm4_human Human Yes 5.6 EC50 = 2300 Funct
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
460 5 2 8 2.6 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NCC4=CC=C(C=C4)S(=O)(=O)N)C
CHEMBL3810300 acm4_human Human No 5.6 EC50 = 2300 Funct
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
381 3 0 6 5.0 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CC5=C(C=C4)OCC5)C
CHEMBL3809384 acm4_human Human Yes 5.6 EC50 = 2300 Funct
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
460 5 2 8 2.6 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NCC4=CC=C(C=C4)S(=O)(=O)N)C
CHEMBL3809384 acm4_human Human Yes 5.6 EC50 = 2344.2 Funct
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
460 5 2 8 2.6 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NCC4=CC=C(C=C4)S(=O)(=O)N)C
CHEMBL2057391 acm4_human Human Yes 5.6 EC50 = 2344.2 Funct
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
299 3 1 5 2.8 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=CN=CC=C3
CHEMBL2057391 acm4_human Human Yes 5.6 EC50 = 2344.2 Funct
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
299 3 1 5 2.8 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)C3=CN=CC=C3
CHEMBL3616499 acm4_human Human No 6.6 EC50 = 235 Funct
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
446 6 2 4 3.7 CC1=CC=C(C=C1)C(=O)NC2C(CC3=C2C=C(C=C3)N=C(C)N(C)CC4=CC=C(C=C4)F)O
CHEMBL3616499 acm4_human Human No 6.6 EC50 = 235 Funct
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
446 6 2 4 3.7 CC1=CC=C(C=C1)C(=O)NC2C(CC3=C2C=C(C=C3)N=C(C)N(C)CC4=CC=C(C=C4)F)O
CHEMBL304142 acm4_human Human Yes 6.6 EC50 = 240 Funct
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)
168 1 1 4 0.3 COC1=NOC2=C1CNCCC2
CHEMBL2313397 acm4_human Human No 6.6 EC50 = 249 Funct
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
353 3 2 6 3.6 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=NC=CS3)N
CHEMBL1223753 acm4_human Human Yes 6.6 EC50 = 251.2 Funct
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
333 2 1 4 2.2 CC1=CC2=C(C=C1F)NC(=O)N2C3CCN(CC3)C4CCOCC4
CHEMBL1223753 acm4_human Human Yes 6.6 EC50 = 251.2 Funct
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
333 2 1 4 2.2 CC1=CC2=C(C=C1F)NC(=O)N2C3CCN(CC3)C4CCOCC4
CHEMBL2313388 acm4_human Human No 6.6 EC50 = 271 Funct
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
348 3 2 6 2.9 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=NC=NC=C3)N
CHEMBL1084941 acm4_rat Rat No 5.6 EC50 = 2710 Funct
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)
317 3 0 3 2.3 CN1C=C(C=N1)C2=CC=C(C=C2)CN3C4=CC=CC=C4C(=O)C3=O
CHEMBL1084941 acm4_rat Rat No 5.6 EC50 = 2710 Funct
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)
317 3 0 3 2.3 CN1C=C(C=N1)C2=CC=C(C=C2)CN3C4=CC=CC=C4C(=O)C3=O
CHEMBL2057416 acm4_human Human Yes 5.6 EC50 = 2818.4 Funct
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
285 3 1 5 2.4 COC1=C2C(=CC=C1)SC(=N2)NC(=O)C3=CC=NC=C3
CHEMBL2057416 acm4_human Human Yes 5.6 EC50 = 2818.4 Funct
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
285 3 1 5 2.4 COC1=C2C(=CC=C1)SC(=N2)NC(=O)C3=CC=NC=C3
CHEMBL2313370 acm4_human Human No 6.5 EC50 = 289 Funct
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
340 2 2 5 3.5 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC3CCOCC3)N
CHEMBL2336059 acm4_human Human No 7.5 EC50 = 29 Funct
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
398 5 0 4 2.8 CCOC(=O)N1C2CCC1CC(C2)CN3CCC(C3)N4C(=O)CC5=CC=CC=C54
CHEMBL2313387 acm4_human Human No 6.5 EC50 = 294 Funct
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
348 3 2 6 2.5 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=NC=CN=C3)N
CHEMBL69306 acm4_human Human No 7.5 EC50 = 30 Funct
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)
192 2 1 4 0.4 C#CCOC1=NOC2=C1CNCCC2
CHEMBL3354067 acm4_human Human No 7.5 EC50 = 30.9 Funct
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
538 12 0 7 4.9 CN1CCC=C(C1)C2=NSN=C2OCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354067 acm4_human Human No 7.5 EC50 = 30.9 Funct
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
538 12 0 7 4.9 CN1CCC=C(C1)C2=NSN=C2OCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL1242979 acm4_human Human No 6.5 EC50 = 300 Funct
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
502 9 1 7 3.3 COC1=C(C=C(C=C1)CC(=O)NC2CCN(CC2)CCCN3C(=O)CCC4=CC(=C(C=C43)F)F)OC
CHEMBL1212989 acm4_rat Rat No 6.5 EC50 = 300 Funct
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
329 3 2 5 4.0 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)F)N)C
CHEMBL1242979 acm4_human Human No 6.5 EC50 = 300 Funct
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
502 9 1 7 3.3 COC1=C(C=C(C=C1)CC(=O)NC2CCN(CC2)CCCN3C(=O)CCC4=CC(=C(C=C43)F)F)OC
CHEMBL1212989 acm4_rat Rat No 6.5 EC50 = 300 Funct
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
329 3 2 5 4.0 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)F)N)C
CHEMBL2313385 acm4_human Human No 4.5 EC50 = 30000 Funct
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
361 4 2 5 4.0 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCCC3=CN=CC=C3)N
CHEMBL2313371 acm4_human Human No 6.5 EC50 = 307 Funct
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
312 2 2 4 4.1 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC(C)(C)C)N
CHEMBL1223804 acm4_human Human No 7.5 EC50 = 31.6 Funct
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
371 4 0 3 3.6 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C(=O)CC4=C3C=C(C=C4)C
CHEMBL1223804 acm4_human Human No 7.5 EC50 = 31.6 Funct
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
371 4 0 3 3.6 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C(=O)CC4=C3C=C(C=C4)C
CHEMBL2336057 acm4_human Human No 6.5 EC50 = 320 Funct
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
387 5 1 5 1.1 CCOC(=O)N1CCC(CC1)(CN2CCC(C2)N3C(=O)CC4=CC=CC=C43)O
CHEMBL2313390 acm4_human Human No 6.5 EC50 = 326 Funct
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
348 3 2 6 2.5 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CN=NC=C3)N
CHEMBL3354068 acm4_human Human No 7.5 EC50 = 35.5 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354068 acm4_human Human No 7.5 EC50 = 35.5 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3618444 acm4_human Human No 6.5 EC50 = 355 Funct
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
496 6 3 4 3.9 CC(=NCC1=CC(=CC=C1)F)NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL3618444 acm4_human Human No 6.5 EC50 = 355 Funct
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
496 6 3 4 3.9 CC(=NCC1=CC(=CC=C1)F)NC2=CC3=C(CC(C3NC(=O)C4=CC=C(C=C4)Br)O)C=C2
CHEMBL2313382 acm4_human Human No 6.5 EC50 = 356 Funct
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
347 3 2 5 3.5 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CC=CC=N3)N
CHEMBL3618447 acm4_human Human No 5.4 EC50 = 3720 Funct
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
510 6 2 4 4.1 CC(=NC1=CC2=C(CC(C2NC(=O)C3=CC=C(C=C3)Br)O)C=C1)N(C)CC4=CC=C(C=C4)F
CHEMBL3618447 acm4_human Human No 5.4 EC50 = 3720 Funct
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
510 6 2 4 4.1 CC(=NC1=CC2=C(CC(C2NC(=O)C3=CC=C(C=C3)Br)O)C=C1)N(C)CC4=CC=C(C=C4)F
CHEMBL1314270 acm4_human Human Yes 5.4 EC50 = 3800 Funct
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
435 3 1 5 5.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=C(C=CC(=C4)Cl)Cl)C
CHEMBL1314270 acm4_human Human Yes 5.4 EC50 = 3801.9 Funct
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
435 3 1 5 5.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=C(C=CC(=C4)Cl)Cl)C
CHEMBL1314270 acm4_human Human Yes 5.4 EC50 = 3801.9 Funct
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
435 3 1 5 5.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=C(C=CC(=C4)Cl)Cl)C
CHEMBL3808920 acm4_human Human Yes 6.4 EC50 = 389.1 Funct
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
410 4 2 6 3.0 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)C(=O)N)C
CHEMBL3808920 acm4_human Human Yes 6.4 EC50 = 389.1 Funct
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
410 4 2 6 3.0 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)C(=O)N)C
CHEMBL1223803 acm4_human Human No 7.4 EC50 = 39.8 Funct
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
385 5 0 3 4.2 CCCOC1CCC(CC1)(C)N2CCC(CC2)N3C(=O)CC4=C3C=C(C=C4)C
CHEMBL1223803 acm4_human Human No 7.4 EC50 = 39.8 Funct
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
385 5 0 3 4.2 CCCOC1CCC(CC1)(C)N2CCC(CC2)N3C(=O)CC4=C3C=C(C=C4)C
CHEMBL3808920 acm4_human Human Yes 6.4 EC50 = 390 Funct
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
410 4 2 6 3.0 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)C(=O)N)C
CHEMBL342400 acm4_human Human No 5.4 EC50 = 3900 Funct
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
421 7 0 10 1.6 CN1CCC=C(C1)C2=NSN=C2OCCOC3=NSN=C3C4=CCCN(C4)C
CHEMBL3618449 acm4_human Human No 6.4 EC50 = 392 Funct
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
450 6 2 5 3.5 CC(=NC1=CC2=C(CC(C2NC(=O)C3=CC=C(C=C3)F)O)C=C1)N(C)CC4=CC=C(C=C4)F
CHEMBL3618449 acm4_human Human No 6.4 EC50 = 392 Funct
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
450 6 2 5 3.5 CC(=NC1=CC2=C(CC(C2NC(=O)C3=CC=C(C=C3)F)O)C=C1)N(C)CC4=CC=C(C=C4)F
CHEMBL3616500 acm4_human Human No 6.4 EC50 = 393 Funct
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
500 6 2 7 4.3 CC(=NC1=CC2=C(CC(C2NC(=O)C3=CC=C(C=C3)C(F)(F)F)O)C=C1)N(C)CC4=CC=C(C=C4)F
CHEMBL3616500 acm4_human Human No 6.4 EC50 = 393 Funct
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
500 6 2 7 4.3 CC(=NC1=CC2=C(CC(C2NC(=O)C3=CC=C(C=C3)C(F)(F)F)O)C=C1)N(C)CC4=CC=C(C=C4)F
CHEMBL143466 acm4_human Human No 8.3 EC50 = 4.7 Funct
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
579 16 0 10 6.8 CN1CCC=C(C1)C2=NSN=C2SCCCCCCCCCCCSC3=NSN=C3C4=CCCN(C4)C
CHEMBL1212994 acm4_rat Rat Yes 6.4 EC50 = 400 Funct
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
346 3 2 4 4.6 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)Cl)N)C
CHEMBL1212994 acm4_rat Rat Yes 6.4 EC50 = 400 Funct
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
346 3 2 4 4.6 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)Cl)N)C
CHEMBL3618450 acm4_human Human No 6.4 EC50 = 405 Funct
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
466 6 2 4 4.0 CC(=NC1=CC2=C(CC(C2NC(=O)C3=CC=C(C=C3)Cl)O)C=C1)N(C)CC4=CC=C(C=C4)F
CHEMBL3618450 acm4_human Human No 6.4 EC50 = 405 Funct
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
466 6 2 4 4.0 CC(=NC1=CC2=C(CC(C2NC(=O)C3=CC=C(C=C3)Cl)O)C=C1)N(C)CC4=CC=C(C=C4)F
CHEMBL1357034 acm4_human Human Yes 6.4 EC50 = 410 Funct
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
446 4 2 8 2.7 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)S(=O)(=O)N)C
CHEMBL2313372 acm4_human Human No 6.4 EC50 = 418 Funct
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
328 5 2 5 3.3 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCCCOC)N
CHEMBL3810183 acm4_human Human No 5.4 EC50 = 4265.8 Funct
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
375 3 0 6 4.9 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CN=C(C=C4)Cl)C
CHEMBL3810183 acm4_human Human No 5.4 EC50 = 4265.8 Funct
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
375 3 0 6 4.9 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CN=C(C=C4)Cl)C
CHEMBL3810183 acm4_human Human No 5.4 EC50 = 4300 Funct
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
375 3 0 6 4.9 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CN=C(C=C4)Cl)C
CHEMBL3808442 acm4_human Human No 5.4 EC50 = 4365.2 Funct
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
355 3 0 7 3.7 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CN=C(N=C4)C)C
CHEMBL3808442 acm4_human Human No 5.4 EC50 = 4365.2 Funct
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
355 3 0 7 3.7 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CN=C(N=C4)C)C
CHEMBL3808442 acm4_human Human No 5.4 EC50 = 4400 Funct
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
355 3 0 7 3.7 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)OC4=CN=C(N=C4)C)C
CHEMBL335542 acm4_human Human No 8.3 EC50 = 5.2 Funct
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
553 16 0 13 1.2 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCOC3=NSN=C3C4=CCCN(C4)C
CHEMBL134641 acm4_human Human Yes 8.2 EC50 = 5.7 Funct
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
193 2 0 4 1.0 CON=C(C#N)C1CN2CCC1CC2
CHEMBL1589763 acm4_human Human No 6.3 EC50 = 500 Funct
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
440 6 2 8 4.5 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=C(C(=CC=C3)F)F)N)OCC4=CC=NC=C4
CHEMBL1223806 acm4_human Human No 6.3 EC50 = 501.2 Funct
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
358 3 0 4 3.6 CC1=CC2=C(C=C1)OC(=O)N2C3CCN(CC3)C4(CCC(CC4)OC)C
CHEMBL1223939 acm4_human Human No 6.3 EC50 = 501.2 Funct
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
451 6 0 6 3.4 CCCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=CC(=C4)S(=O)(=O)C)OC3=O
CHEMBL1223753 acm4_human Human Yes 6.3 EC50 = 501.2 Funct
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
333 2 1 4 2.2 CC1=CC2=C(C=C1F)NC(=O)N2C3CCN(CC3)C4CCOCC4
CHEMBL1223806 acm4_human Human No 6.3 EC50 = 501.2 Funct
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
358 3 0 4 3.6 CC1=CC2=C(C=C1)OC(=O)N2C3CCN(CC3)C4(CCC(CC4)OC)C
CHEMBL1223939 acm4_human Human No 6.3 EC50 = 501.2 Funct
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
451 6 0 6 3.4 CCCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=CC(=C4)S(=O)(=O)C)OC3=O
CHEMBL1223753 acm4_human Human Yes 6.3 EC50 = 501.2 Funct
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
333 2 1 4 2.2 CC1=CC2=C(C=C1F)NC(=O)N2C3CCN(CC3)C4CCOCC4
CHEMBL2313402 acm4_human Human No 7.3 EC50 = 52 Funct
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
326 2 2 5 3.1 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC3CCOC3)N
CHEMBL1978713 acm4_human Human Yes 6.3 EC50 = 520 Funct
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
341 4 2 5 3.9 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)OC)N)C
CHEMBL59898 acm4_human Human Yes 7.3 EC50 = 54 Funct
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
392 4 1 5 3.9 CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=C(C=C5)OC)C
CHEMBL59898 acm4_human Human Yes 7.3 EC50 = 54 Funct
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
392 4 1 5 3.9 CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=C(C=C5)OC)C
CHEMBL2057417 acm4_human Human No 7.3 EC50 = 56 Funct
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
347 3 2 5 3.5 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CC=NC=C3)N
CHEMBL1455259 acm4_human Human Yes 6.2 EC50 = 570 Funct
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
424 4 2 6 3.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)C(=O)NC)C
CHEMBL1455259 acm4_human Human Yes 6.2 EC50 = 575.4 Funct
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
424 4 2 6 3.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)C(=O)NC)C
CHEMBL3808485 acm4_human Human No 6.2 EC50 = 575.4 Funct
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
338 3 0 6 3.6 CC1=NC=C(C=C1)OC2CCN(CC2)C3=NC=NC4=C3C=C(C=C4)F
CHEMBL1455259 acm4_human Human Yes 6.2 EC50 = 575.4 Funct
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
424 4 2 6 3.4 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)C(=O)NC)C
CHEMBL3808485 acm4_human Human No 6.2 EC50 = 575.4 Funct
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
338 3 0 6 3.6 CC1=NC=C(C=C1)OC2CCN(CC2)C3=NC=NC4=C3C=C(C=C4)F
CHEMBL3808485 acm4_human Human No 6.2 EC50 = 600 Funct
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
338 3 0 6 3.6 CC1=NC=C(C=C1)OC2CCN(CC2)C3=NC=NC4=C3C=C(C=C4)F
CHEMBL3809096 acm4_human Human No 6.2 EC50 = 600 Funct
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
354 3 0 6 4.3 CC1=NC=C(C=C1)OC2CCN(CC2)C3=C4C(=C(SC4=NC=N3)C)C
CHEMBL2313378 acm4_human Human No 6.2 EC50 = 600 Funct
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
361 3 2 5 3.9 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC(C)C3=CC=NC=C3)N
CHEMBL1212982 acm4_rat Rat Yes 5.2 EC50 = 6000 Funct
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
263 2 2 4 3.2 CC1=CC(=NC2=C1C(=C(S2)C(=O)NC(C)C)N)C
CHEMBL1212982 acm4_rat Rat Yes 5.2 EC50 = 6000 Funct
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
263 2 2 4 3.2 CC1=CC(=NC2=C1C(=C(S2)C(=O)NC(C)C)N)C
CHEMBL3809096 acm4_human Human No 6.2 EC50 = 602.6 Funct
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
354 3 0 6 4.3 CC1=NC=C(C=C1)OC2CCN(CC2)C3=C4C(=C(SC4=NC=N3)C)C
CHEMBL3809096 acm4_human Human No 6.2 EC50 = 602.6 Funct
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
354 3 0 6 4.3 CC1=NC=C(C=C1)OC2CCN(CC2)C3=C4C(=C(SC4=NC=N3)C)C
CHEMBL2313379 acm4_human Human No 7.2 EC50 = 61 Funct
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
361 3 2 5 3.9 CC1=NC=CC(=C1)CNC(=O)C2=C(C3=C(C(=C(N=C3S2)C)Cl)C)N
CHEMBL3808847 acm4_human Human Yes 5.2 EC50 = 6166.0 Funct
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
451 4 2 6 3.1 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)N5CCNC5=O)C
CHEMBL3808847 acm4_human Human Yes 5.2 EC50 = 6166.0 Funct
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
451 4 2 6 3.1 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)N5CCNC5=O)C
CHEMBL1978713 acm4_human Human Yes 6.2 EC50 = 620 Funct
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
341 4 2 5 3.9 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)OC)N)C
CHEMBL3808847 acm4_human Human Yes 5.2 EC50 = 6200 Funct
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
451 4 2 6 3.1 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)N5CCNC5=O)C
CHEMBL2146599 acm4_human Human Yes 6.2 EC50 = 631.0 Funct
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
315 2 1 3 2.7 CC1=CC2=C(C=C1)NC(=O)N2C3CCN(CC3)C4CCOCC4
CHEMBL2146599 acm4_human Human Yes 6.2 EC50 = 631.0 Funct
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
315 2 1 3 2.7 CC1=CC2=C(C=C1)NC(=O)N2C3CCN(CC3)C4CCOCC4
CHEMBL965 acm4_human Human Yes 5.2 EC50 = 6606.9 Funct
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
147 4 1 2 -0.4 C[N+](C)(C)CCOC(=O)N
CHEMBL965 acm4_human Human Yes 5.2 EC50 = 6606.9 Funct
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
147 4 1 2 -0.4 C[N+](C)(C)CCOC(=O)N
CHEMBL3354069 acm4_human Human No 4.2 EC50 = 66069.3 Funct
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
594 16 0 7 7.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354069 acm4_human Human No 4.2 EC50 = 66069.3 Funct
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
594 16 0 7 7.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL2313381 acm4_human Human No 6.2 EC50 = 669 Funct
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
361 3 2 5 3.9 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC(C)C3=CN=CC=C3)N
CHEMBL69305 acm4_human Human No 7.2 EC50 = 67 Funct
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)
182 2 1 4 0.7 CCOC1=NOC2=C1CNCCC2
CHEMBL3809076 acm4_human Human No 6.2 EC50 = 690 Funct
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
351 3 0 5 4.4 CC1=NC=C(C=C1)OC2CCN(CC2)C3=CC(=NC4=C3C=C(C=C4)F)C
CHEMBL3809076 acm4_human Human No 6.2 EC50 = 691.8 Funct
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
351 3 0 5 4.4 CC1=NC=C(C=C1)OC2CCN(CC2)C3=CC(=NC4=C3C=C(C=C4)F)C
CHEMBL3809076 acm4_human Human No 6.2 EC50 = 691.8 Funct
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
351 3 0 5 4.4 CC1=NC=C(C=C1)OC2CCN(CC2)C3=CC(=NC4=C3C=C(C=C4)F)C
CHEMBL3354067 acm4_human Human No 5.2 EC50 = 7079.5 Funct
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
538 12 0 7 4.9 CN1CCC=C(C1)C2=NSN=C2OCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL2057406 acm4_human Human Yes 5.2 EC50 = 7079.5 Funct
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
305 3 2 4 3.3 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)NC3CCCC3
CHEMBL3354067 acm4_human Human No 5.2 EC50 = 7079.5 Funct
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
538 12 0 7 4.9 CN1CCC=C(C1)C2=NSN=C2OCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL2057406 acm4_human Human Yes 5.2 EC50 = 7079.5 Funct
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
305 3 2 4 3.3 CC1=C2C(=C(C=C1)OC)N=C(S2)NC(=O)NC3CCCC3
CHEMBL1212992 acm4_rat Rat No 6.2 EC50 = 715 Funct
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
379 3 2 7 4.8 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)C(F)(F)F)N)C
CHEMBL1212992 acm4_rat Rat No 6.2 EC50 = 715 Funct
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
379 3 2 7 4.8 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)C(F)(F)F)N)C
CHEMBL2313377 acm4_human Human No 7.1 EC50 = 77 Funct
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
296 2 2 4 3.6 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NC3CC3)N
CHEMBL2057683 acm4_human Human No 5.1 EC50 = 7762.5 Funct
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
262 3 1 4 2.9 CC1=C2C(=C(C=C1)OC)N=C(S2)C(=O)NC3CC3
CHEMBL2057683 acm4_human Human No 5.1 EC50 = 7762.5 Funct
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
262 3 1 4 2.9 CC1=C2C(=C(C=C1)OC)N=C(S2)C(=O)NC3CC3
CHEMBL1223941 acm4_human Human No 6.1 EC50 = 794.3 Funct
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
414 6 0 6 2.9 CC1(CCC(CC1)OCCOC)N2CCC(CC2)N3C4=C(C=CC(=C4)C#N)OC3=O
CHEMBL1223863 acm4_human Human No 6.1 EC50 = 794.3 Funct
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
383 4 0 5 3.4 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=CC(=C4)C#N)OC3=O
CHEMBL1223941 acm4_human Human No 6.1 EC50 = 794.3 Funct
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
414 6 0 6 2.9 CC1(CCC(CC1)OCCOC)N2CCC(CC2)N3C4=C(C=CC(=C4)C#N)OC3=O
CHEMBL1223863 acm4_human Human No 6.1 EC50 = 794.3 Funct
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
383 4 0 5 3.4 CCOC1CCC(CC1)(C)N2CCC(CC2)N3C4=C(C=CC(=C4)C#N)OC3=O
CHEMBL2313391 acm4_human Human No 7.1 EC50 = 80 Funct
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
390 3 2 6 4.4 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=CC4=C(C=C3)OCO4)N
CHEMBL2313389 acm4_human Human No 6.1 EC50 = 810 Funct
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
348 3 2 6 2.9 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCC3=NC=CC=N3)N
CHEMBL3809482 acm4_human Human No 6.1 EC50 = 812.8 Funct
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
377 2 0 6 3.2 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCSCC4)C
CHEMBL3809482 acm4_human Human No 6.1 EC50 = 812.8 Funct
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
377 2 0 6 3.2 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCSCC4)C
CHEMBL3809482 acm4_human Human No 6.1 EC50 = 820 Funct
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
377 2 0 6 3.2 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCSCC4)C
CHEMBL2111051 acm4_human Human Yes 6.1 EC50 = 844 Funct
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
165 2 0 2 0.8 C#CCOC1CN2CCC1CC2
CHEMBL2111051 acm4_human Human Yes 6.1 EC50 = 844 Funct
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
165 2 0 2 0.8 C#CCOC1CN2CCC1CC2
CHEMBL2313386 acm4_human Human No 6.1 EC50 = 844 Funct
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
361 4 2 5 4.0 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCCC3=CC=CC=N3)N
CHEMBL3808592 acm4_human Human Yes 6.1 EC50 = 850 Funct
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
445 4 1 7 3.3 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)S(=O)(=O)C)C
CHEMBL3808592 acm4_human Human Yes 6.1 EC50 = 851.1 Funct
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
445 4 1 7 3.3 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)S(=O)(=O)C)C
CHEMBL3808592 acm4_human Human Yes 6.1 EC50 = 851.1 Funct
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
445 4 1 7 3.3 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)NC4=CC=C(C=C4)S(=O)(=O)C)C
CHEMBL3633184 acm4_human Human No 7.1 EC50 = 86 Funct
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
413 5 1 4 2.6 CCOC(=O)N1C2CCC1CC(C2)CN3CCC(C3)N4CC5=CC=CC=C5NC4=O
CHEMBL3633184 acm4_human Human No 7.1 EC50 = 86 Funct
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
413 5 1 4 2.6 CCOC(=O)N1C2CCC1CC(C2)CN3CCC(C3)N4CC5=CC=CC=C5NC4=O
CHEMBL485913 acm4_human Human No 8.0 EC50 = 9.1 Funct
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 receptor
387 6 2 5 1.9 C1CN(CCC1N2CCC(CC2)N3C4=CC=CC=C4NC3=O)CCOC(=O)N
CHEMBL491209 acm4_human Human No 8.0 EC50 = 9.1 Funct
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 receptor
372 4 1 4 2.8 CCOC(=O)N1CCC(CC1)N2CCC(CC2)N3C4=CC=CC=C4NC3=O
CHEMBL485913 acm4_human Human No 8.0 EC50 = 9.1 Funct
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 receptor
387 6 2 5 1.9 C1CN(CCC1N2CCC(CC2)N3C4=CC=CC=C4NC3=O)CCOC(=O)N
CHEMBL491209 acm4_human Human No 8.0 EC50 = 9.1 Funct
Agonist activity at muscarinic M4 receptorAgonist activity at muscarinic M4 receptor
372 4 1 4 2.8 CCOC(=O)N1CCC(CC1)N2CCC(CC2)N3C4=CC=CC=C4NC3=O
CHEMBL1589763 acm4_rat Rat No 6.1 EC50 = 900 Funct
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
440 6 2 8 4.5 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=C(C(=CC=C3)F)F)N)OCC4=CC=NC=C4
CHEMBL2313373 acm4_human Human No 6.0 EC50 = 926 Funct
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
367 4 2 5 4.0 CC1=C2C(=C(SC2=NC(=C1Cl)C)C(=O)NCCC3CCCN3C)N
CHEMBL3289440 acm4_human Human No 7.0 EC50 = 93 Funct
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
437 5 0 7 1.7 CCOC(=O)N1CCC(CC1)CN2CCC3(CC2)CN(C4=C3C=CC=N4)S(=O)(=O)C
CHEMBL3289440 acm4_human Human No 7.0 EC50 = 93 Funct
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
437 5 0 7 1.7 CCOC(=O)N1CCC(CC1)CN2CCC3(CC2)CN(C4=C3C=CC=N4)S(=O)(=O)C
CHEMBL1589763 acm4_rat Rat No 7.0 EC50 = 95.3 Funct
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)
440 6 2 8 4.5 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=C(C(=CC=C3)F)F)N)OCC4=CC=NC=C4
CHEMBL1589763 acm4_rat Rat No 7.0 EC50 = 95.3 Funct
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)
440 6 2 8 4.5 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=C(C(=CC=C3)F)F)N)OCC4=CC=NC=C4
CHEMBL3808485 acm4_rat Rat No 6.0 EC50 = 950 Funct
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
338 3 0 6 3.6 CC1=NC=C(C=C1)OC2CCN(CC2)C3=NC=NC4=C3C=C(C=C4)F
CHEMBL3808485 acm4_rat Rat No 6.0 EC50 = 950 Funct
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
338 3 0 6 3.6 CC1=NC=C(C=C1)OC2CCN(CC2)C3=NC=NC4=C3C=C(C=C4)F
CHEMBL3809378 acm4_human Human Yes 6.0 EC50 = 955.0 Funct
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
485 3 0 7 3.9 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCCC5=C4C=CC(=C5)S(=O)(=O)C)C
CHEMBL3809378 acm4_human Human Yes 6.0 EC50 = 955.0 Funct
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
485 3 0 7 3.9 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCCC5=C4C=CC(=C5)S(=O)(=O)C)C
CHEMBL3809378 acm4_human Human Yes 6.0 EC50 = 960 Funct
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
485 3 0 7 3.9 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCCC5=C4C=CC(=C5)S(=O)(=O)C)C
CHEMBL3808983 acm4_human Human No 6.0 EC50 = 970 Funct
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
362 2 0 6 3.3 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCC(C4)F)C
CHEMBL3808983 acm4_human Human No 6.0 EC50 = 977.2 Funct
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
362 2 0 6 3.3 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCC(C4)F)C
CHEMBL3808983 acm4_human Human No 6.0 EC50 = 977.2 Funct
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
362 2 0 6 3.3 CC1=C(SC2=NC=NC(=C12)N3CCC(CC3)C(=O)N4CCC(C4)F)C
CHEMBL1551487 acm4_rat Rat No 7.0 EC50 = 100.0 Funct
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)
435 7 2 7 4.2 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)OC)N)OCC4=CC=NC=C4
CHEMBL1551487 acm4_rat Rat No 7.0 EC50 = 100.0 Funct
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)
435 7 2 7 4.2 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)OC)N)OCC4=CC=NC=C4
CHEMBL1187846 acm4_human Human No 9.2 IC50 = 0.6 Funct
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
303 5 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4
CHEMBL9967 acm4_human Human Yes 8.9 IC50 = 1.1 Funct
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
351 2 1 5 0.1 CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL9967 acm4_human Human Yes 8.9 IC50 = 1.1 Funct
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
351 2 1 5 0.1 CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL1187846 acm4_human Human No 8.9 IC50 = 1.3 Funct
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
303 5 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4
CHEMBL1187846 acm4_human Human No 8.9 IC50 = 1.3 Funct
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
303 5 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4
CHEMBL1231 acm4_human Human Yes 8.7 IC50 = 2.0 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
357 8 1 4 4.2 CCN(CC)CC#CCOC(=O)C(C1CCCCC1)(C2=CC=CC=C2)O
CHEMBL1231 acm4_human Human Yes 8.7 IC50 = 2.0 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
357 8 1 4 4.2 CCN(CC)CC#CCOC(=O)C(C1CCCCC1)(C2=CC=CC=C2)O
CHEMBL477542 acm4_human Human No 8.0 IC50 = 10 Funct
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
327 14 5 4 -0.7 C(CCCCN=C(N)N)CCCC(=O)C(CCCN=C(N)N)N
CHEMBL477542 acm4_human Human No 8.0 IC50 = 10 Funct
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
327 14 5 4 -0.7 C(CCCCN=C(N)N)CCCC(=O)C(CCCN=C(N)N)N
CHEMBL15936 acm4_human Human No 4.0 IC50 = 100000 Funct
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
191 0 1 4 1.2 C1CNCC2=C1C=CC3=NSN=C23
CHEMBL499519 acm4_human Human No 6.0 IC50 = 1040 Funct
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 receptor expressed in insect Sf9 cells
758 23 5 11 6.2 CCCCCCCCCCCC(C(C)C(=O)NC1CCCCN(C1=O)O)OC(=O)C(CCCCN(C(=O)C)O)NC(=O)C2=COC(=C3C=CC=CC3=O)N2
CHEMBL9967 acm4_human Human Yes 6.0 IC50 = 1047.1 Funct
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
351 2 1 5 0.1 CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL9967 acm4_human Human Yes 6.0 IC50 = 1047.1 Funct
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
351 2 1 5 0.1 CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL9967 acm4_human Human Yes 6.0 IC50 = 1047.1 Funct
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
351 2 1 5 0.1 CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL9967 acm4_human Human Yes 6.0 IC50 = 1047.1 Funct
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
351 2 1 5 0.1 CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL64000 acm4_rat Rat No 8.0 IC50 = 11 Funct
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
169 2 1 3 0.9 CC(=O)OC1CC2CCCC1N2
CHEMBL132698 acm4_human Human No 6.0 IC50 = 1100 Funct
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
154 2 0 3 0.5 CON=CC1CN2CCC1C2
CHEMBL104 acm4_human Human Yes 4.9 IC50 = 11756 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
345 4 0 1 5.0 C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CN=C4
CHEMBL104 acm4_human Human Yes 4.9 IC50 = 11756 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
345 4 0 1 5.0 C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CN=C4
CHEMBL1201207 acm4_human Human Yes 4.9 IC50 = 11924 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
472 4 4 9 0.1 CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)COP(=O)(O)O)O)C)O)F)C
CHEMBL1201207 acm4_human Human Yes 4.9 IC50 = 11924 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
472 4 4 9 0.1 CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)COP(=O)(O)O)O)C)O)F)C
CHEMBL216927 acm4_human Human Yes 7.9 IC50 = 12.6 Funct
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
488 16 0 13 1.2 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCOC3=NSN=C3OC
CHEMBL216927 acm4_human Human Yes 7.9 IC50 = 12.6 Funct
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
488 16 0 13 1.2 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCOC3=NSN=C3OC
CHEMBL15944 acm4_human Human No 5.9 IC50 = 1200 Funct
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
227 2 0 5 1.5 CN1CCC=C(C1)C2=NSN=C2SC
CHEMBL3354073 acm4_human Human No 4.9 IC50 = 12302.7 Funct
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
359 9 1 3 3.5 C1CN(CCC1CCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354073 acm4_human Human No 4.9 IC50 = 12302.7 Funct
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
359 9 1 3 3.5 C1CN(CCC1CCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL900 acm4_human Human Yes 6.9 IC50 = 125 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
269 6 0 2 3.8 CC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C
CHEMBL900 acm4_human Human Yes 6.9 IC50 = 125 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
269 6 0 2 3.8 CC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C
CHEMBL216928 acm4_human Human No 5.9 IC50 = 1258.9 Funct
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
488 16 0 13 2.1 CN1CCC=CC1C2=NSN=C2OCCOCCOCCOCCOC3=NC(=NS3)OC
CHEMBL216928 acm4_human Human No 5.9 IC50 = 1258.9 Funct
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
488 16 0 13 2.1 CN1CCC=CC1C2=NSN=C2OCCOCCOCCOCCOC3=NC(=NS3)OC
CHEMBL461571 acm4_human Human No 5.9 IC50 = 1340 Funct
Displacement of radioligand from muscarinic M4 receptorDisplacement of radioligand from muscarinic M4 receptor
532 8 1 8 7.1 CC1=C(C2=C(N1CC3=CC(=CC=C3)OC(C)C(=O)O)C=C(C=C2)OC(F)(F)F)C(=O)C4=CC=C(C=C4)Cl
CHEMBL461571 acm4_human Human No 5.9 IC50 = 1340 Funct
Displacement of radioligand from muscarinic M4 receptorDisplacement of radioligand from muscarinic M4 receptor
532 8 1 8 7.1 CC1=C(C2=C(N1CC3=CC(=CC=C3)OC(C)C(=O)O)C=C(C=C2)OC(F)(F)F)C(=O)C4=CC=C(C=C4)Cl
CHEMBL7303 acm4_human Human Yes 4.9 IC50 = 13500 Funct
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
155 2 0 3 0.3 CN1CCC=C(C1)C(=O)OC
CHEMBL728 acm4_human Human Yes 5.9 IC50 = 1363 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
374 4 0 4 4.9 CN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL1180284 acm4_human Human No 4.9 IC50 = 13692 Funct
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
245 4 0 3 2.1 CCN1CCC(=C(C1)C(=O)OC)C2=CC=CC=C2
CHEMBL395110 acm4_human Human Yes 6.9 IC50 = 137 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
310 2 0 3 5.6 CN1CCCC(C1)CN2C3=CC=CC=C3SC4=CC=CC=C42
CHEMBL1306 acm4_human Human Yes 4.9 IC50 = 13714 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
532 8 0 7 4.8 CC(C)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=NC=N4)C5=C(C=C(C=C5)Cl)Cl
CHEMBL1180285 acm4_human Human No 6.9 IC50 = 138 Funct
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
349 7 0 3 4.4 CCN1CCC(=C(C1)C(=O)OCCC2=CC=C(C=C2)C)C3=CC=CC=C3
CHEMBL2164905 acm4_human Human No 6.9 IC50 = 140 Funct
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
326 4 0 3 3.4 CN1CCN(CC1)C(=O)C(CC2=CC=CC=C2)(C3=CC=CC=C3)F
CHEMBL3354068 acm4_human Human No 6.8 IC50 = 144.5 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354068 acm4_human Human No 6.8 IC50 = 144.5 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL15675 acm4_human Human No 4.8 IC50 = 14500 Funct
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
225 0 0 5 0.6 CN1CCC2=C(C1)C3=NSN=C3SC2
CHEMBL304036 acm4_human Human No 5.8 IC50 = 1474.8 Funct
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
376 3 1 4 4.3 CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=CC=C5C)C
CHEMBL3354074 acm4_human Human No 5.8 IC50 = 1479.1 Funct
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
387 11 1 3 4.6 C1CN(CCC1CCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354074 acm4_human Human No 5.8 IC50 = 1479.1 Funct
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
387 11 1 3 4.6 C1CN(CCC1CCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL71 acm4_human Human Yes 6.8 IC50 = 149 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
319 4 0 3 5.2 CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl
CHEMBL61494 acm4_human Human No 5.8 IC50 = 1498.3 Funct
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
408 5 1 6 3.5 CCOC(=O)C1=CNC2=C1C3=C(C=C2)OC4C5=CC(=C(C=C5CCN4C3)OC)OC
CHEMBL3808906 acm4_human Human No 5.8 IC50 = 1500 Funct
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
410 6 0 6 5.7 CCCCN(C1CCN(CC1)C2=C3C(=C(SC3=NC=N2)C)C)C4=CN=C(C=C4)C
CHEMBL1090097 acm4_human Human No 5.8 IC50 = 1500 Funct
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
480 4 1 9 5.5 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3=C(C=CC(=C3)C(F)(F)F)C(F)(F)F)Cl
CHEMBL3808906 acm4_human Human No 5.8 IC50 = 1500 Funct
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
410 6 0 6 5.7 CCCCN(C1CCN(CC1)C2=C3C(=C(SC3=NC=N2)C)C)C4=CN=C(C=C4)C
CHEMBL1090097 acm4_human Human No 5.8 IC50 = 1500 Funct
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
480 4 1 9 5.5 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3=C(C=CC(=C3)C(F)(F)F)C(F)(F)F)Cl
CHEMBL715 acm4_human Human Yes 6.8 IC50 = 155 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
312 1 1 5 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL715 acm4_human Human Yes 6.8 IC50 = 155 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
312 1 1 5 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL481 acm4_human Human Yes 5.8 IC50 = 1556 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
587 5 1 8 3.0 CCC1=C2C=C(C=CC2=NC3=C1CN4C3=CC5=C(C4=O)COC(=O)C5(CC)O)OC(=O)N6CCC(CC6)N7CCCCC7
CHEMBL120972 acm4_human Human No 5.8 IC50 = 1577.9 Funct
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
358 12 0 3 6.0 CCCCCCCCCOC(=O)C1CN(CC=C1C2=CC=CC=C2)CC
CHEMBL244946 acm4_human Human Yes 6.8 IC50 = 158.5 Funct
Antagonist activity at human muscarinic receptor M4Antagonist activity at human muscarinic receptor M4
538 7 0 6 5.4 CC1=NC2=CC=CC(=C2C=C1)C3=NN=C(N3C)SCCCN4CCC5=C(CC4)C=C(C=C5)C6=CC(=NN6C)C
CHEMBL1083925 acm4_human Human No 6.8 IC50 = 158.5 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
361 4 2 3 4.3 CC1CNCCC1CNC(=O)C2=C(C=CC=C2F)C3=CC(=CC=C3)Cl
CHEMBL244946 acm4_human Human Yes 6.8 IC50 = 158.5 Funct
Antagonist activity at human muscarinic receptor M4Antagonist activity at human muscarinic receptor M4
538 7 0 6 5.4 CC1=NC2=CC=CC(=C2C=C1)C3=NN=C(N3C)SCCCN4CCC5=C(CC4)C=C(C=C5)C6=CC(=NN6C)C
CHEMBL1083925 acm4_human Human No 6.8 IC50 = 158.5 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
361 4 2 3 4.3 CC1CNCCC1CNC(=O)C2=C(C=CC=C2F)C3=CC(=CC=C3)Cl
CHEMBL55 acm4_human Human Yes 5.8 IC50 = 1580 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
340 10 4 4 2.6 C1=CC(=CC=C1C(=N)N)OCCCCCOC2=CC=C(C=C2)C(=N)N
CHEMBL1083108 acm4_human Human No 5.8 IC50 = 1584.9 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
347 4 2 3 3.9 C1CNCCC1CNC(=O)C2=CC=CC=C2C3=C(C=CC(=C3)Cl)F
CHEMBL1083108 acm4_human Human No 5.8 IC50 = 1584.9 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
347 4 2 3 3.9 C1CNCCC1CNC(=O)C2=CC=CC=C2C3=C(C=CC(=C3)Cl)F
CHEMBL3354073 acm4_human Human No 5.8 IC50 = 1621.8 Funct
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
359 9 1 3 3.5 C1CN(CCC1CCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354073 acm4_human Human No 5.8 IC50 = 1621.8 Funct
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
359 9 1 3 3.5 C1CN(CCC1CCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL7002 acm4_human Human Yes 4.8 IC50 = 16224 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
333 5 1 4 4.8 CC1(CCCCC1)COC2=CC=C(C=C2)CC3C(=O)NC(=O)S3
CHEMBL7002 acm4_human Human Yes 4.8 IC50 = 16224 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
333 5 1 4 4.8 CC1(CCCCC1)COC2=CC=C(C=C2)CC3C(=O)NC(=O)S3
CHEMBL62247 acm4_human Human No 5.8 IC50 = 1624 Funct
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
406 5 1 5 4.2 CCOC1=CC2=C(C=C1)C3N(CC2)CC4=C(O3)C=CC5=C4C(=C(N5)C)C(=O)OCC
CHEMBL954 acm4_human Human Yes 5.8 IC50 = 1651 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
406 9 0 2 7.2 CCN(CC)CCOC1=CC=C(C=C1)C(=C(C2=CC=CC=C2)Cl)C3=CC=CC=C3
CHEMBL954 acm4_human Human Yes 5.8 IC50 = 1651 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
406 9 0 2 7.2 CCN(CC)CCOC1=CC=C(C=C1)C(=C(C2=CC=CC=C2)Cl)C3=CC=CC=C3
CHEMBL1113 acm4_human Human Yes 5.8 IC50 = 1737 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
314 1 1 3 2.6 C1CN(CCN1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl
CHEMBL1113 acm4_human Human Yes 5.8 IC50 = 1737 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
314 1 1 3 2.6 C1CN(CCN1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl
CHEMBL255169 acm4_rat Rat Yes 4.8 IC50 = 18000 Funct
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
372 6 1 3 3.9 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)CCC3=CC=CC=C3)Cl
CHEMBL255169 acm4_rat Rat Yes 4.8 IC50 = 18000 Funct
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
372 6 1 3 3.9 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)CCC3=CC=CC=C3)Cl
CHEMBL296419 acm4_human Human Yes 5.7 IC50 = 1861 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
459 8 1 5 6.0 COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
CHEMBL296419 acm4_human Human Yes 5.7 IC50 = 1861 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
459 8 1 5 6.0 COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
CHEMBL3354068 acm4_human Human No 5.7 IC50 = 1862.1 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354068 acm4_human Human No 5.7 IC50 = 1862.1 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL7568 acm4_human Human Yes 5.7 IC50 = 1983 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
400 9 1 4 6.0 CCN(CC)CCCC(C)NC1=C2C=C(C=CC2=NC3=C1C=CC(=C3)Cl)OC
CHEMBL7568 acm4_human Human Yes 5.7 IC50 = 1983 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
400 9 1 4 6.0 CCN(CC)CCCC(C)NC1=C2C=C(C=CC2=NC3=C1C=CC(=C3)Cl)OC
CHEMBL1123 acm4_human Human Yes 8.5 IC50 = 2.9 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 8 0 3 5.5 CCN(CC)CCOC(=O)C1(CCCCC1)C2CCCCC2
CHEMBL1123 acm4_human Human Yes 8.5 IC50 = 2.9 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 8 0 3 5.5 CCN(CC)CCOC(=O)C1(CCCCC1)C2CCCCC2
CHEMBL1626 acm4_human Human Yes 7.7 IC50 = 20 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
344 6 0 2 5.0 CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCC3CCCN3C
CHEMBL1626 acm4_human Human Yes 7.7 IC50 = 20 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
344 6 0 2 5.0 CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCC3CCCN3C
CHEMBL271704 acm4_rat Rat No 4.7 IC50 = 20000 Funct
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
384 5 1 3 3.9 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3CC3C4=CC=CC=C4)Cl
CHEMBL271704 acm4_rat Rat No 4.7 IC50 = 20000 Funct
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
384 5 1 3 3.9 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3CC3C4=CC=CC=C4)Cl
CHEMBL62251 acm4_human Human No 5.7 IC50 = 2050 Funct
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
406 4 1 5 4.3 CC1=C(C2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OC(C)C
CHEMBL808 acm4_human Human Yes 5.7 IC50 = 2122 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
382 6 0 2 5.3 C1=CC(=CC=C1COC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl)Cl
CHEMBL333940 acm4_human Human No 5.7 IC50 = 2123.9 Funct
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
372 13 0 3 6.6 CCCCCCCCCCOC(=O)C1CN(CC=C1C2=CC=CC=C2)CC
CHEMBL3808947 acm4_human Human No 5.6 IC50 = 2400 Funct
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
396 5 0 6 5.4 CCCN(C1CCN(CC1)C2=C3C(=C(SC3=NC=N2)C)C)C4=CN=C(C=C4)C
CHEMBL3808947 acm4_human Human No 5.6 IC50 = 2400 Funct
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
396 5 0 6 5.4 CCCN(C1CCN(CC1)C2=C3C(=C(SC3=NC=N2)C)C)C4=CN=C(C=C4)C
CHEMBL490 acm4_human Human Yes 6.6 IC50 = 244 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
329 4 1 5 3.5 C1CNCC(C1C2=CC=C(C=C2)F)COC3=CC4=C(C=C3)OCO4
CHEMBL3354069 acm4_human Human No 5.6 IC50 = 2454.7 Funct
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
594 16 0 7 7.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354069 acm4_human Human No 5.6 IC50 = 2454.7 Funct
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
594 16 0 7 7.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL9967 acm4_human Human Yes 6.6 IC50 = 246.8 Funct
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
351 2 1 5 0.1 CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL1200604 acm4_human Human Yes 7.6 IC50 = 25 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 6 1 3 1.5 CCN(CC1=CC=NC=C1)C(=O)C(CO)C2=CC=CC=C2
CHEMBL1200604 acm4_human Human Yes 7.6 IC50 = 25 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 6 1 3 1.5 CCN(CC1=CC=NC=C1)C(=O)C(CO)C2=CC=CC=C2
CHEMBL216983 acm4_human Human No 4.6 IC50 = 25118.9 Funct
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
373 13 1 9 -0.2 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCO
CHEMBL216983 acm4_human Human No 4.6 IC50 = 25118.9 Funct
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
373 13 1 9 -0.2 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCO
CHEMBL809 acm4_human Human Yes 5.6 IC50 = 2630.9 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
306 2 1 1 4.8 CNC1CCC(C2=CC=CC=C12)C3=CC(=C(C=C3)Cl)Cl
CHEMBL61700 acm4_human Human No 5.6 IC50 = 2633.7 Funct
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
455 5 1 5 5.4 CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=C(C=C5)OC6=CC=CC=C6)C
CHEMBL936 acm4_human Human Yes 6.6 IC50 = 271 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 6 1 2 4.2 C1CCN(CC1)CCCC(C2=CC=CC=C2)(C3=CC=CC=C3)O
CHEMBL936 acm4_human Human Yes 6.6 IC50 = 271 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 6 1 2 4.2 C1CCN(CC1)CCCC(C2=CC=CC=C2)(C3=CC=CC=C3)O
CHEMBL121059 acm4_human Human No 6.6 IC50 = 282.3 Funct
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
358 12 0 3 6.0 CCCCCCCCCOC(=O)C1=C(CCN(C1)CC)C2=CC=CC=C2
CHEMBL564 acm4_human Human Yes 6.5 IC50 = 299 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 4 0 3 4.5 CN(C)CCCN1C2=CC=CC=C2SC3=CC=CC=C31
CHEMBL564 acm4_human Human Yes 6.5 IC50 = 299 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 4 0 3 4.5 CN(C)CCCN1C2=CC=CC=C2SC3=CC=CC=C31
CHEMBL1187846 acm4_human Human No 8.4 IC50 = 3.8 Funct
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
303 5 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4
CHEMBL1187846 acm4_human Human No 8.4 IC50 = 3.8 Funct
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
303 5 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4
CHEMBL1187846 acm4_human Human No 8.4 IC50 = 3.8 Funct
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
303 5 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4
CHEMBL1187846 acm4_human Human No 8.4 IC50 = 3.8 Funct
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
303 5 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4
CHEMBL1770373 acm4_human Human Yes 6.5 IC50 = 300 Funct
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
239 2 1 3 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL1770373 acm4_human Human Yes 6.5 IC50 = 300 Funct
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
239 2 1 3 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL58228 acm4_human Human No 6.5 IC50 = 301.1 Funct
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
422 5 1 6 3.9 CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=CC(=C(C=C5CCN4C3)OC)OC)C
CHEMBL2024407 acm4_human Human No 5.5 IC50 = 3100 Funct
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
345 7 2 4 2.2 CCOC(=O)N1C2CCC1CC(C2)NCCNC(=O)C3=CC=CC=C3
CHEMBL2024408 acm4_human Human No 5.5 IC50 = 3100 Funct
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
345 7 2 4 2.2 CCOC(=O)N1C2CCC1CC(C2)NCCNC(=O)C3=CC=CC=C3
CHEMBL2024407 acm4_human Human No 5.5 IC50 = 3100 Funct
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
345 7 2 4 2.2 CCOC(=O)N1C2CCC1CC(C2)NCCNC(=O)C3=CC=CC=C3
CHEMBL2024408 acm4_human Human No 5.5 IC50 = 3100 Funct
Antagonist activity at human muscarinic M4 receptor by calcium mobilization assayAntagonist activity at human muscarinic M4 receptor by calcium mobilization assay
345 7 2 4 2.2 CCOC(=O)N1C2CCC1CC(C2)NCCNC(=O)C3=CC=CC=C3
CHEMBL1084993 acm4_human Human No 5.5 IC50 = 3162.3 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
343 4 2 2 4.2 CC1CNCCC1CNC(=O)C2=CC=CC=C2C3=CC(=CC=C3)Cl
CHEMBL1082365 acm4_human Human No 5.5 IC50 = 3162.3 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
379 4 2 4 4.3 CC1CNCCC1(CNC(=O)C2=C(C=CC=C2F)C3=CC(=CC=C3)Cl)F
CHEMBL1084993 acm4_human Human No 5.5 IC50 = 3162.3 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
343 4 2 2 4.2 CC1CNCCC1CNC(=O)C2=CC=CC=C2C3=CC(=CC=C3)Cl
CHEMBL1082365 acm4_human Human No 5.5 IC50 = 3162.3 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
379 4 2 4 4.3 CC1CNCCC1(CNC(=O)C2=C(C=CC=C2F)C3=CC(=CC=C3)Cl)F
CHEMBL91 acm4_human Human Yes 5.5 IC50 = 3197 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
416 6 0 2 5.3 C1=CC(=C(C=C1Cl)Cl)COC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl
CHEMBL91 acm4_human Human Yes 5.5 IC50 = 3197 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
416 6 0 2 5.3 C1=CC(=C(C=C1Cl)Cl)COC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl
CHEMBL3354073 acm4_human Human No 5.5 IC50 = 3311.3 Funct
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
359 9 1 3 3.5 C1CN(CCC1CCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354073 acm4_human Human No 5.5 IC50 = 3311.3 Funct
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
359 9 1 3 3.5 C1CN(CCC1CCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL60142 acm4_human Human No 6.5 IC50 = 333.5 Funct
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
378 4 1 5 3.5 CCOC(=O)C1=CNC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=C(C=C5)OC
CHEMBL1172 acm4_human Human Yes 6.5 IC50 = 339 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
311 0 1 2 4.5 C1CC2=C(C=CC(=C2)Cl)C(=C3CCNCC3)C4=C1C=CC=N4
CHEMBL3354067 acm4_human Human No 6.5 IC50 = 354.8 Funct
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
538 12 0 7 4.9 CN1CCC=C(C1)C2=NSN=C2OCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354067 acm4_human Human No 6.5 IC50 = 354.8 Funct
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
538 12 0 7 4.9 CN1CCC=C(C1)C2=NSN=C2OCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL61412 acm4_human Human No 6.4 IC50 = 359.6 Funct
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
406 5 1 5 4.4 CCCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=C(C=C5)OC)C
CHEMBL75880 acm4_human Human Yes 5.5 IC50 = 3591.9 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
277 4 1 1 6.8 C1CCC(CC1)C(CC2CCCCN2)C3CCCCC3
CHEMBL75880 acm4_human Human Yes 5.5 IC50 = 3591.9 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
277 4 1 1 6.8 C1CCC(CC1)C(CC2CCCCN2)C3CCCCC3
CHEMBL633 acm4_human Human Yes 5.4 IC50 = 3630 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
645 11 0 4 7.6 CCCCC1=C(C2=CC=CC=C2O1)C(=O)C3=CC(=C(C(=C3)I)OCCN(CC)CC)I
CHEMBL3354075 acm4_human Human No 5.4 IC50 = 3630.8 Funct
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
415 13 1 3 5.7 C1CN(CCC1CCCCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354075 acm4_human Human No 5.4 IC50 = 3630.8 Funct
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
415 13 1 3 5.7 C1CN(CCC1CCCCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL43064 acm4_human Human Yes 5.4 IC50 = 3660 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
369 6 0 2 5.8 C1CN(CCN1CC=CC2=CC=CC=C2)C(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL1090759 acm4_human Human No 5.4 IC50 = 3700 Funct
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
480 4 1 9 5.5 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)Cl
CHEMBL1090096 acm4_human Human No 5.4 IC50 = 3700 Funct
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
412 4 1 6 4.6 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3=CC(=CC=C3)C(F)(F)F)Cl
CHEMBL1092461 acm4_human Human Yes 5.4 IC50 = 3700 Funct
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
358 4 1 3 4.1 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3=CC=C(C=C3)C)Cl
CHEMBL1090759 acm4_human Human No 5.4 IC50 = 3700 Funct
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
480 4 1 9 5.5 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)Cl
CHEMBL1090096 acm4_human Human No 5.4 IC50 = 3700 Funct
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
412 4 1 6 4.6 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3=CC(=CC=C3)C(F)(F)F)Cl
CHEMBL1092461 acm4_human Human Yes 5.4 IC50 = 3700 Funct
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
358 4 1 3 4.1 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3=CC=C(C=C3)C)Cl
CHEMBL301041 acm4_human Human No 5.4 IC50 = 3713.8 Funct
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
362 3 1 4 3.9 CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=CC=CC=C5CCN4C3)C
CHEMBL657 acm4_human Human Yes 6.4 IC50 = 372 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
255 6 0 2 3.3 CN(C)CCOC(C1=CC=CC=C1)C2=CC=CC=C2
CHEMBL1108 acm4_human Human Yes 5.4 IC50 = 3849 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
379 6 1 4 3.5 C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F
CHEMBL1108 acm4_human Human Yes 5.4 IC50 = 3849 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
379 6 1 4 3.5 C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F
CHEMBL1221 acm4_human Human Yes 5.4 IC50 = 3958 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
398 6 0 2 6.1 C1=CC(=CC=C1CSC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl)Cl
CHEMBL1221 acm4_human Human Yes 5.4 IC50 = 3958 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
398 6 0 2 6.1 C1=CC(=CC=C1CSC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl)Cl
CHEMBL386983 acm4_human Human No 6.4 IC50 = 398.1 Funct
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
532 19 0 14 1.1 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCOCCOC3=NSN=C3OC
CHEMBL1083723 acm4_human Human No 6.4 IC50 = 398.1 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
343 4 2 2 4.1 CC1=C(C=C(C=C1)C2=CC=CC=C2C(=O)NCC3CCNCC3)Cl
CHEMBL386983 acm4_human Human No 6.4 IC50 = 398.1 Funct
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
532 19 0 14 1.1 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCOCCOC3=NSN=C3OC
CHEMBL1083723 acm4_human Human No 6.4 IC50 = 398.1 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
343 4 2 2 4.1 CC1=C(C=C(C=C1)C2=CC=CC=C2C(=O)NCC3CCNCC3)Cl
CHEMBL3354068 acm4_human Human No 6.4 IC50 = 407.4 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354068 acm4_human Human No 6.4 IC50 = 407.4 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL21731 acm4_human Human Yes 6.4 IC50 = 413 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
277 4 1 1 4.6 CNCCCC12CCC(C3=CC=CC=C31)C4=CC=CC=C24
CHEMBL21731 acm4_human Human Yes 6.4 IC50 = 413 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
277 4 1 1 4.6 CNCCCC12CCC(C3=CC=CC=C31)C4=CC=CC=C24
CHEMBL1180343 acm4_human Human No 4.4 IC50 = 42313 Funct
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
365 8 0 4 4.0 CCN1CCC(=C(C1)C(=O)OCCC2=CC=C(C=C2)OC)C3=CC=CC=C3
CHEMBL120135 acm4_human Human No 5.4 IC50 = 4246.3 Funct
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
315 5 0 3 4.2 CCN1CCC(C(C1)C(=O)OC2CCCCC2)C3=CC=CC=C3
CHEMBL3354067 acm4_human Human No 6.4 IC50 = 446.7 Funct
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
538 12 0 7 4.9 CN1CCC=C(C1)C2=NSN=C2OCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354067 acm4_human Human No 6.4 IC50 = 446.7 Funct
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
538 12 0 7 4.9 CN1CCC=C(C1)C2=NSN=C2OCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL42 acm4_human Human Yes 7.4 IC50 = 45 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL42 acm4_human Human Yes 7.4 IC50 = 45 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL588119 acm4_human Human Yes 5.3 IC50 = 4561 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
338 12 2 3 5.8 CCCCCCCCNC(C)C(C1=CC=C(C=C1)SC(C)C)O
CHEMBL303758 acm4_human Human No 6.3 IC50 = 464.8 Funct
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
376 3 1 4 4.3 CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=C(C=C5)C)C
CHEMBL12587 acm4_rat Rat Yes 6.3 IC50 = 470 Funct
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
174 2 1 2 0.1 CC1C(CC(O1)C[N+](C)(C)C)O
CHEMBL59347 acm4_human Human No 5.3 IC50 = 4741.3 Funct
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
350 2 1 4 3.6 CC1=CC2=C(N1)C=CC3=C2CN4CCC5=CC(=C(C=C5C4O3)OC)OC
CHEMBL7303 acm4_human Human Yes 4.3 IC50 = 47500 Funct
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
155 2 0 3 0.3 CN1CCC=C(C1)C(=O)OC
CHEMBL83 acm4_human Human Yes 5.3 IC50 = 4817 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
372 8 0 2 7.1 CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3
CHEMBL135645 acm4_human Human No 7.3 IC50 = 49 Funct
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
193 2 0 4 0.9 CON=C(C#N)C12CCCN(C1)CC2
CHEMBL344892 acm4_human Human No 6.3 IC50 = 495 Funct
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
179 2 0 4 0.5 CON=C(C#N)C12CCN(C1)CC2
CHEMBL480464 acm4_human Human No 6.3 IC50 = 498 Funct
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
255 6 1 4 2.2 CCC(C)C(C(=O)OCC1CCN2C1CCC2)O
CHEMBL480464 acm4_human Human No 6.3 IC50 = 498 Funct
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
255 6 1 4 2.2 CCC(C)C(C(=O)OCC1CCN2C1CCC2)O
CHEMBL1187846 acm4_human Human No 8.3 IC50 = 5.4 Funct
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
303 5 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4
CHEMBL59939 acm4_human Human No 6.3 IC50 = 501 Funct
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
378 3 1 5 3.5 CC1=C(C2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OC
CHEMBL1085507 acm4_human Human No 5.3 IC50 = 5011.9 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
329 4 2 2 3.8 C1CNCCC1CNC(=O)C2=CC=CC=C2C3=CC(=CC=C3)Cl
CHEMBL1085507 acm4_human Human No 5.3 IC50 = 5011.9 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
329 4 2 2 3.8 C1CNCCC1CNC(=O)C2=CC=CC=C2C3=CC(=CC=C3)Cl
CHEMBL256202 acm4_rat Rat Yes 5.3 IC50 = 5100 Funct
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
338 7 1 3 3.9 CCCCCC(=O)NC1=CC(=C(C=C1)N2CCN(CC2)CC)Cl
CHEMBL256202 acm4_rat Rat Yes 5.3 IC50 = 5100 Funct
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
338 7 1 3 3.9 CCCCCC(=O)NC1=CC(=C(C=C1)N2CCN(CC2)CC)Cl
CHEMBL2315675 acm4_rat Rat No 5.3 IC50 = 5128.6 Funct
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
423 4 1 4 3.8 CC1=CC=CC=C1CN2CCC(CC2)N3CCC(C(C3)F)N4C5=CC=CC=C5NC4=O
CHEMBL30008 acm4_human Human Yes 5.3 IC50 = 5656 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
405 6 0 4 6.0 C1CN(CCN1CC=CC2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
CHEMBL332320 acm4_human Human No 6.3 IC50 = 566.2 Funct
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
372 13 0 3 6.6 CCCCCCCCCCOC(=O)C1=C(CCN(C1)CC)C2=CC=CC=C2
CHEMBL3354074 acm4_human Human No 6.2 IC50 = 588.8 Funct
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
387 11 1 3 4.6 C1CN(CCC1CCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354075 acm4_human Human No 6.2 IC50 = 588.8 Funct
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
415 13 1 3 5.7 C1CN(CCC1CCCCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354074 acm4_human Human No 6.2 IC50 = 588.8 Funct
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
387 11 1 3 4.6 C1CN(CCC1CCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354075 acm4_human Human No 6.2 IC50 = 588.8 Funct
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
415 13 1 3 5.7 C1CN(CCC1CCCCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL300987 acm4_human Human No 5.2 IC50 = 6027.8 Funct
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
392 4 1 5 3.9 CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=CC(=C5)OC)C
CHEMBL3354067 acm4_human Human No 6.2 IC50 = 631.0 Funct
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
538 12 0 7 4.9 CN1CCC=C(C1)C2=NSN=C2OCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354067 acm4_human Human No 6.2 IC50 = 631.0 Funct
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
538 12 0 7 4.9 CN1CCC=C(C1)C2=NSN=C2OCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL219118 acm4_human Human No 5.2 IC50 = 6309.6 Funct
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
468 16 0 12 3.2 COC1=NSC(=N1)OCCCOCCCOCCCOC2=NSN=C2C3=CN=CC=C3
CHEMBL219118 acm4_human Human No 5.2 IC50 = 6309.6 Funct
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
468 16 0 12 3.2 COC1=NSC(=N1)OCCCOCCCOCCCOC2=NSN=C2C3=CN=CC=C3
CHEMBL58 acm4_human Human Yes 6.2 IC50 = 644.1 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
444 12 8 10 1.0 C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO
CHEMBL58 acm4_human Human Yes 6.2 IC50 = 644.1 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
444 12 8 10 1.0 C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO
CHEMBL271519 acm4_rat Rat Yes 4.2 IC50 = 66000 Funct
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
344 4 1 3 4.1 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3=CC=CC=C3)Cl
CHEMBL271519 acm4_rat Rat Yes 4.2 IC50 = 66000 Funct
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
344 4 1 3 4.1 CCN1CCN(CC1)C2=C(C=C(C=C2)NC(=O)C3=CC=CC=C3)Cl
CHEMBL1770373 acm4_human Human Yes 5.2 IC50 = 6800 Funct
Antagonist activity at human muscarinic M4 receptorAntagonist activity at human muscarinic M4 receptor
239 2 1 3 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL1770373 acm4_human Human Yes 5.2 IC50 = 6800 Funct
Antagonist activity at human muscarinic M4 receptorAntagonist activity at human muscarinic M4 receptor
239 2 1 3 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL643 acm4_human Human Yes 8.1 IC50 = 7.6 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 3 0 3 4.8 CC(CN1C2=CC=CC=C2SC3=CC=CC=C31)N(C)C
CHEMBL978 acm4_rat Rat Yes 6.2 IC50 = 700 Funct
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
160 4 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C
CHEMBL2391353 acm4_human Human No 4.1 IC50 = 73000 Funct
Binding affinity to M4 receptor (unknown origin) by radioligand displacement assayBinding affinity to M4 receptor (unknown origin) by radioligand displacement assay
265 3 1 3 1.8 C1CCC(CC1)NC(=O)CN2CCN3CCCC3C2
CHEMBL270580 acm4_rat Rat Yes 5.1 IC50 = 7900 Funct
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
416 8 1 4 4.9 CCCCOC1=CC=CC(=C1)C(=O)NC2=CC(=C(C=C2)N3CCN(CC3)CC)Cl
CHEMBL270580 acm4_rat Rat Yes 5.1 IC50 = 7900 Funct
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
416 8 1 4 4.9 CCCCOC1=CC=CC(=C1)C(=O)NC2=CC(=C(C=C2)N3CCN(CC3)CC)Cl
CHEMBL3354074 acm4_human Human No 6.1 IC50 = 794.3 Funct
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
387 11 1 3 4.6 C1CN(CCC1CCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354074 acm4_human Human No 6.1 IC50 = 794.3 Funct
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
387 11 1 3 4.6 C1CN(CCC1CCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL218755 acm4_human Human No 5.1 IC50 = 7943.3 Funct
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
444 13 0 12 1.4 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOC3=NSN=C3OC
CHEMBL373888 acm4_human Human No 5.1 IC50 = 7943.3 Funct
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
399 10 0 11 1.5 CN1CCC=C(C1)C2=NSN=C2OCCOCCOC3=NSN=C3OC
CHEMBL1083618 acm4_human Human No 5.1 IC50 = 7943.3 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
345 4 2 3 3.2 C1CNCC=C1CNC(=O)C2=C(C=CC=C2F)C3=CC(=CC=C3)Cl
CHEMBL218755 acm4_human Human No 5.1 IC50 = 7943.3 Funct
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
444 13 0 12 1.4 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOC3=NSN=C3OC
CHEMBL373888 acm4_human Human No 5.1 IC50 = 7943.3 Funct
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
399 10 0 11 1.5 CN1CCC=C(C1)C2=NSN=C2OCCOCCOC3=NSN=C3OC
CHEMBL1083618 acm4_human Human No 5.1 IC50 = 7943.3 Funct
Inhibition of human muscarinic M4 receptor expressed in CHO cellsInhibition of human muscarinic M4 receptor expressed in CHO cells
345 4 2 3 3.2 C1CNCC=C1CNC(=O)C2=C(C=CC=C2F)C3=CC(=CC=C3)Cl
CHEMBL479 acm4_human Human Yes 7.1 IC50 = 80 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
371 4 0 4 5.9 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)SC
CHEMBL137384 acm4_human Human No 6.1 IC50 = 800 Funct
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
179 2 0 4 0.6 CON=C(C#N)C1CN2CCC1C2
CHEMBL341447 acm4_human Human No 5.1 IC50 = 8000 Funct
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
267 4 0 2 2.5 C[N+](C)(C)CC#CCOC(=O)C1=CC(=CC=C1)Cl
CHEMBL3354075 acm4_human Human No 6.1 IC50 = 812.8 Funct
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
415 13 1 3 5.7 C1CN(CCC1CCCCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354075 acm4_human Human No 6.1 IC50 = 812.8 Funct
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
415 13 1 3 5.7 C1CN(CCC1CCCCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL305660 acm4_human Human Yes 6.1 IC50 = 827.9 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
470 10 0 3 7.2 CC(C)(C)C1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)OC(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL305660 acm4_human Human Yes 6.1 IC50 = 827.9 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
470 10 0 3 7.2 CC(C)(C)C1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)OC(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL648 acm4_human Human Yes 6.1 IC50 = 852 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
266 3 0 2 3.6 CN1CCN(CC1)C(C2=CC=CC=C2)C3=CC=CC=C3
CHEMBL648 acm4_human Human Yes 6.1 IC50 = 852 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
266 3 0 2 3.6 CN1CCN(CC1)C(C2=CC=CC=C2)C3=CC=CC=C3
CHEMBL134641 acm4_human Human Yes 7.1 IC50 = 90 Funct
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
193 2 0 4 1.0 CON=C(C#N)C1CN2CCC1CC2
CHEMBL59898 acm4_human Human Yes 7.0 IC50 = 90.7 Funct
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
392 4 1 5 3.9 CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=C(C=C5)OC)C
CHEMBL415 acm4_human Human Yes 7.0 IC50 = 91 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
315 4 0 2 5.2 CN(C)CCCN1C2=CC=CC=C2CCC3=C1C=C(C=C3)Cl
CHEMBL415 acm4_human Human Yes 7.0 IC50 = 91 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
315 4 0 2 5.2 CN(C)CCCN1C2=CC=CC=C2CCC3=C1C=C(C=C3)Cl
CHEMBL479224 acm4_human Human No 6.0 IC50 = 910 Funct
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
370 15 5 4 -0.4 CC(=O)NC(CCCN=C(N)N)C(=O)CCCCCCCCN=C(N)N
CHEMBL479224 acm4_human Human No 6.0 IC50 = 910 Funct
Displacement of QNB from muscarinic M4 receptorDisplacement of QNB from muscarinic M4 receptor
370 15 5 4 -0.4 CC(=O)NC(CCCN=C(N)N)C(=O)CCCCCCCCN=C(N)N
CHEMBL445 acm4_human Human Yes 7.0 IC50 = 95 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
263 3 1 1 4.5 CNCCC=C1C2=CC=CC=C2CCC3=CC=CC=C31
CHEMBL445 acm4_human Human Yes 7.0 IC50 = 95 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
263 3 1 1 4.5 CNCCC=C1C2=CC=CC=C2CCC3=CC=CC=C31
CHEMBL3354069 acm4_human Human No 4.0 IC50 = 95499.3 Funct
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
594 16 0 7 7.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354069 acm4_human Human No 4.0 IC50 = 95499.3 Funct
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
594 16 0 7 7.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL294726 acm4_human Human No 5.0 IC50 = 9735.2 Funct
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
320 1 1 3 3.7 CC1=CC2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC
CHEMBL135328 acm4_human Human No 6.0 IC50 = 975 Funct
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
179 2 0 4 0.6 CON=C(C#N)C1CN2CCC1C2
CHEMBL61774 acm4_human Human No 5.0 IC50 = 9927.5 Funct
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
348 2 1 4 3.5 CC1=C(C2=C(N1)C=CC3=C2CN4CCC5=CC=CC=C5C4O3)C(=O)OC
CHEMBL127587 acm4_rat Rat No 8.6 Kd = 2.4 Funct
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
427 6 1 4 3.2 C1CN2CCC1C(C2)OC(=O)C(CC=CI)(C3=CC=CC=C3)O
CHEMBL71124 acm4_human Human No 10.2 Ki = 0.1 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
426 6 0 4 5.9 CC(C1CCN(CC1)C2CCCCC2)C3=CC=C(C=C3)S(=O)C4=CC=C(C=C4)OC
CHEMBL2114068 acm4_human Human No 10.1 Ki = 0.1 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
424 6 0 4 6.1 COC1=CC=C(C=C1)S(=O)C2=CC=C(C=C2)C(=C)C3CCN(CC3)C4CCCCC4
CHEMBL1910856 acm4_human Human Yes 9.9 Ki = 0.1 Funct
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
445 9 2 4 4.8 CC(C)(CCC(C1=CC=CC=C1)(C2=CC=CC=C2)C(=O)N)N3CC(C3)OC4=CC=CC(=C4)O
CHEMBL1910856 acm4_human Human Yes 9.9 Ki = 0.1 Funct
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
445 9 2 4 4.8 CC(C)(CCC(C1=CC=CC=C1)(C2=CC=CC=C2)C(=O)N)N3CC(C3)OC4=CC=CC(=C4)O
CHEMBL1231 acm4_human Human Yes 9.6 Ki = 0.3 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
357 8 1 4 4.2 CCN(CC)CC#CCOC(=O)C(C1CCCCC1)(C2=CC=CC=C2)O
CHEMBL2115128 acm4_human Human No 9.5 Ki = 0.3 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
424 6 0 4 6.1 COC1=CC=C(C=C1)S(=O)C2=CC=C(C=C2)C(=C)C3CCN(CC3)C4CCCCC4
CHEMBL71147 acm4_human Human No 9.5 Ki = 0.3 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
440 6 0 4 6.1 COC1=CC=C(C=C1)S(=O)(=O)C2=CC=C(C=C2)C(=C)C3CCN(CC3)C4CCCCC4
CHEMBL3629360 acm4_human Human No 9.5 Ki = 0.4 Funct
Antagonist activity at muscarinic M4 receptor (unknown origin)Antagonist activity at muscarinic M4 receptor (unknown origin)
705 14 5 8 5.4 C1CCC(CC1)C(C2=CC=CC=C2)(C3=NN(C=N3)CC4CCN(CC4)CCC5=CC=C(C=C5)CCNCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O)O
CHEMBL3629360 acm4_human Human No 9.5 Ki = 0.4 Funct
Antagonist activity at muscarinic M4 receptor (unknown origin)Antagonist activity at muscarinic M4 receptor (unknown origin)
705 14 5 8 5.4 C1CCC(CC1)C(C2=CC=CC=C2)(C3=NN(C=N3)CC4CCN(CC4)CCC5=CC=C(C=C5)CCNCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O)O
CHEMBL1123 acm4_human Human Yes 9.4 Ki = 0.4 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 8 0 3 5.5 CCN(CC)CCOC(=O)C1(CCCCC1)C2CCCCC2
CHEMBL143469 acm4_human Human No 9.1 Ki = 0.8 Funct
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
519 14 0 10 4.7 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCOC3=NSN=C3C4=CCCN(C4)C
CHEMBL143469 acm4_human Human No 9.1 Ki = 0.8 Funct
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
519 14 0 10 4.7 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCOC3=NSN=C3C4=CCCN(C4)C
CHEMBL3354068 acm4_human Human No 9.1 Ki = 0.9 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354068 acm4_human Human No 9.1 Ki = 0.9 Funct
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
566 14 0 7 6.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL376870 acm4_human Human No 9.0 Ki = 1 Funct
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
332 3 0 3 5.0 CN1CCCC1C2CSC(O2)(C3CCCCC3)C4=CC=CC=C4
CHEMBL326450 acm4_human Human No 9.0 Ki = 1 Funct
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
435 7 1 5 5.2 CCCCC1=C(C2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OCC
CHEMBL376870 acm4_human Human No 9.0 Ki = 1 Funct
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
332 3 0 3 5.0 CN1CCCC1C2CSC(O2)(C3CCCCC3)C4=CC=CC=C4
CHEMBL104693 acm4_human Human No 9.0 Ki = 1 Funct
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.
437 6 1 5 5.2 CCCC1=C(C2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)SC)C(=O)OCC
CHEMBL326450 acm4_human Human No 9.0 Ki = 1 Funct
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.
435 7 1 5 5.2 CCCCC1=C(C2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OCC
CHEMBL643 acm4_human Human Yes 9.0 Ki = 1.1 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 3 0 3 4.8 CC(CN1C2=CC=CC=C2SC3=CC=CC=C31)N(C)C
CHEMBL643 acm4_human Human Yes 9.0 Ki = 1.1 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 3 0 3 4.8 CC(CN1C2=CC=CC=C2SC3=CC=CC=C31)N(C)C
CHEMBL3354069 acm4_human Human No 9.0 Ki = 1.1 Funct
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
594 16 0 7 7.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354069 acm4_human Human No 9.0 Ki = 1.1 Funct
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
594 16 0 7 7.0 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL376255 acm4_human Human No 8.9 Ki = 1.2 Funct
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
332 3 0 3 5.0 CN1CCCC1C2CSC(O2)(C3CCCCC3)C4=CC=CC=C4
CHEMBL376255 acm4_human Human No 8.9 Ki = 1.2 Funct
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
332 3 0 3 5.0 CN1CCCC1C2CSC(O2)(C3CCCCC3)C4=CC=CC=C4
CHEMBL219825 acm4_human Human No 8.9 Ki = 1.3 Funct
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
332 3 0 3 5.0 CN1CCCC1C2CSC(O2)(C3CCCCC3)C4=CC=CC=C4
CHEMBL219825 acm4_human Human No 8.9 Ki = 1.3 Funct
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
332 3 0 3 5.0 CN1CCCC1C2CSC(O2)(C3CCCCC3)C4=CC=CC=C4
CHEMBL131865 acm4_rat Rat No 8.8 Ki = 1.4 Funct
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
650 26 3 7 4.6 CN(CCCCCCCCN(C)CCCCCCNCCCC(=O)N1C2=CC=CC=C2C(=O)NC3=C1N=CC=C3)CCCCCCN
CHEMBL2377267 acm4_human Human No 8.8 Ki = 1.5 Funct
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
339 9 1 5 3.8 CCN(CC)CCOC(=O)C(C1CCCCC1)(C2=CC=CS2)O
CHEMBL286008 acm4_human Human No 8.8 Ki = 1.5 Funct
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
317 8 0 3 5.2 CC(C1CCCCC1)(C2=CC=CC=C2)C(=O)OCCCN(C)C
CHEMBL375073 acm4_human Human No 8.7 Ki = 2.0 Funct
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
325 3 0 3 4.3 CN1CCCC1C2CSC(O2)(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL375073 acm4_human Human No 8.7 Ki = 2.0 Funct
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
325 3 0 3 4.3 CN1CCCC1C2CSC(O2)(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL335542 acm4_human Human No 8.7 Ki = 2.0 Funct
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
553 16 0 13 1.2 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCOC3=NSN=C3C4=CCCN(C4)C
CHEMBL320465 acm4_human Human No 8.7 Ki = 2.0 Funct
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.
421 6 1 5 4.7 CCCC1=C(C2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OCC
CHEMBL106224 acm4_human Human No 8.7 Ki = 2.0 Funct
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.
435 6 0 5 4.6 CCCC1=C(C2=C(N1C)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OCC
CHEMBL280220 acm4_human Human No 8.7 Ki = 2.0 Funct
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.
451 6 0 5 5.2 CCCC1=C(C2=C(N1C)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)SC)C(=O)OCC
CHEMBL205654 acm4_human Human Yes 8.0 Ki = 10 Funct
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
286 4 1 4 3.7 CC1=C(N=C(N=C1NC2CC2)C3CC3)N4CCCCCC4
CHEMBL43383 acm4_rat Rat Yes 8.0 Ki = 10 Funct
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
464 9 1 5 3.1 CCN(CC)CCCCC1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL205654 acm4_human Human Yes 8.0 Ki = 10 Funct
Binding affinity to muscarinic M4 receptorBinding affinity to muscarinic M4 receptor
286 4 1 4 3.7 CC1=C(N=C(N=C1NC2CC2)C3CC3)N4CCCCCC4
CHEMBL104210 acm4_human Human No 8.0 Ki = 11.0 Funct
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.
449 8 1 5 5.8 CCCCCC1=C(C2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OCC
CHEMBL42 acm4_human Human Yes 7.0 Ki = 100 Funct
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL56275 acm4_human Human No 6.0 Ki = 1000 Funct
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
346 2 0 3 5.0 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C
CHEMBL715 acm4_human Human Yes 6.0 Ki = 1000 Funct
Binding affinity to M4 receptor (unknown origin) by PDSP assayBinding affinity to M4 receptor (unknown origin) by PDSP assay
312 1 1 5 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL355769 acm4_human Human No 6.0 Ki = 1000 Funct
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
320 6 0 2 3.5 CC(C)N(C)CCC1=C(C2=CC=CC=C2C1)C(C)C3=CC=CC=N3
CHEMBL1834350 acm4_human Human No 5.0 Ki = 10000 Funct
Inhibition of human muscarinic M4 receptorInhibition of human muscarinic M4 receptor
384 5 2 5 1.2 CCN=C(NS(=O)(=O)C1=CC(=CC=C1)Cl)N2CC3(CCNCC3)C=N2
CHEMBL1834350 acm4_human Human No 5.0 Ki = 10000 Funct
Inhibition of human muscarinic M4 receptorInhibition of human muscarinic M4 receptor
384 5 2 5 1.2 CCN=C(NS(=O)(=O)C1=CC(=CC=C1)Cl)N2CC3(CCNCC3)C=N2
CHEMBL493795 acm4_human Human No 6.0 Ki = 1023.3 Funct
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
341 3 0 4 2.8 CN1CCCC1C2CS(=O)C(O2)(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL168815 acm4_human Human Yes 6.0 Ki = 1023.3 Funct
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
199 0 0 3 1.5 CC1OC2(CN3CCC2CC3)CS1
CHEMBL168815 acm4_human Human Yes 6.0 Ki = 1023.3 Funct
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
199 0 0 3 1.5 CC1OC2(CN3CCC2CC3)CS1
CHEMBL576663 acm4_human Human No 7.0 Ki = 104.7 Funct
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
333 4 1 3 3.7 CN1CCCC1C2=CC=C(O2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O
CHEMBL576663 acm4_human Human No 7.0 Ki = 104.7 Funct
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
333 4 1 3 3.7 CN1CCCC1C2=CC=C(O2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O
CHEMBL305403 acm4_rat Rat No 6.0 Ki = 1040 Funct
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
514 7 3 7 -0.1 C1CN(CCN1CC2=CC=C(C=C2)C(=O)NCCN)CC(=O)N3C4=CC=CC=C4C(=O)NC5=C3N=CC=C5
CHEMBL9967 acm4_human Human Yes 7.0 Ki = 105 Funct
Binding affinity to human M4 muscarinic receptorBinding affinity to human M4 muscarinic receptor
351 2 1 5 0.1 CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL2312376 acm4_human Human No 5.0 Ki = 10500 Funct
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
377 7 0 4 4.0 CCN1CCC(=C(C1)C(=O)OCCC2=CC3=C(C=C2)OCC3)C4=CC=CC=C4
CHEMBL107679 acm4_human Human No 7.0 Ki = 109.7 Funct
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.
421 5 0 5 4.1 CCN1C(=C(C2=C1C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OCC)C
CHEMBL2030626 acm4_human Human No 6.0 Ki = 1098 Funct
Inhibition of M4 muscarinic receptorInhibition of M4 muscarinic receptor
213 2 0 1 2.2 C1CC2CCC1N2CC34C5C6C3C7C6C5C47
CHEMBL2030626 acm4_human Human No 6.0 Ki = 1098 Funct
Inhibition of M4 muscarinic receptorInhibition of M4 muscarinic receptor
213 2 0 1 2.2 C1CC2CCC1N2CC34C5C6C3C7C6C5C47
CHEMBL479 acm4_human Human Yes 8.0 Ki = 11 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
371 4 0 4 5.9 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)SC
CHEMBL214898 acm4_human Human No 8.0 Ki = 11 Funct
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
745 11 2 8 6.6 C1CCC(C1)CN2CCC(CC2)CNC(=O)C3CCCN3C(=O)C4CC(CN4C(=O)CC(C5=CC=C(C=C5)F)(C6=CC=C(C=C6)F)C7=CC=C(C=C7)F)O
CHEMBL2112958 acm4_human Human No 8.0 Ki = 11 Funct
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
663 13 2 4 7.0 C1CCC(CC1)CN2CCCC(C2)CNC(=O)CCNC(=O)C3CCCN3C(=O)CC(C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6
CHEMBL479 acm4_human Human Yes 8.0 Ki = 11 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
371 4 0 4 5.9 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)SC
CHEMBL214898 acm4_human Human No 8.0 Ki = 11 Funct
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
745 11 2 8 6.6 C1CCC(C1)CN2CCC(CC2)CNC(=O)C3CCCN3C(=O)C4CC(CN4C(=O)CC(C5=CC=C(C=C5)F)(C6=CC=C(C=C6)F)C7=CC=C(C=C7)F)O
CHEMBL265256 acm4_human Human Yes 7.9 Ki = 11.5 Funct
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
1124 29 4 13 7.7 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1C2=CC=CC=C2C(=O)NC3=C1N=CC=C3)CC(=O)N4C5=CC=CC=C5C(=O)NC6=C4N=CC=C6)CCCCCCNCC(=O)N7C8=CC=CC=C8C(=O)NC9=C7N=CC=C9
CHEMBL265256 acm4_human Human Yes 7.9 Ki = 11.5 Funct
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
1124 29 4 13 7.7 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1C2=CC=CC=C2C(=O)NC3=C1N=CC=C3)CC(=O)N4C5=CC=CC=C5C(=O)NC6=C4N=CC=C6)CCCCCCNCC(=O)N7C8=CC=CC=C8C(=O)NC9=C7N=CC=C9
CHEMBL265256 acm4_rat Rat Yes 7.9 Ki = 11.5 Funct
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
1124 29 4 13 7.7 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1C2=CC=CC=C2C(=O)NC3=C1N=CC=C3)CC(=O)N4C5=CC=CC=C5C(=O)NC6=C4N=CC=C6)CCCCCCNCC(=O)N7C8=CC=CC=C8C(=O)NC9=C7N=CC=C9
CHEMBL265256 acm4_rat Rat Yes 7.9 Ki = 11.8 Funct
Affinity constant measured against M4 muscarinic receptor rat NG108-15 cellsAffinity constant measured against M4 muscarinic receptor rat NG108-15 cells
1124 29 4 13 7.7 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1C2=CC=CC=C2C(=O)NC3=C1N=CC=C3)CC(=O)N4C5=CC=CC=C5C(=O)NC6=C4N=CC=C6)CCCCCCNCC(=O)N7C8=CC=CC=C8C(=O)NC9=C7N=CC=C9
CHEMBL241283 acm4_human Human No 5.0 Ki = 11000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
423 8 0 4 5.3 CCCCSC1=CCC2=C1C=C(C=C2)N=CN3CCC4=CC(=C(C=C4C3)OC)OC
CHEMBL241283 acm4_human Human No 5.0 Ki = 11000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
423 8 0 4 5.3 CCCCSC1=CCC2=C1C=C(C=C2)N=CN3CCC4=CC(=C(C=C4C3)OC)OC
CHEMBL2205817 acm4_human Human No 6.0 Ki = 1118 Funct
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
280 3 1 3 1.8 C1C2C3C4C1C5C2C6C3C4C5(N6CCC7=CN=CC=C7)O
CHEMBL3354076 acm4_human Human No 7.0 Ki = 112.2 Funct
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
443 15 1 3 6.8 C1CN(CCC1CCCCCCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354076 acm4_human Human No 7.0 Ki = 112.2 Funct
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
443 15 1 3 6.8 C1CN(CCC1CCCCCCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL305660 acm4_human Human Yes 6.9 Ki = 115.5 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
470 10 0 3 7.2 CC(C)(C)C1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)OC(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL2312389 acm4_human Human No 4.9 Ki = 11500 Funct
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
380 9 0 4 4.4 CCN1CCC(=C(C1)C(=O)OCCCC2=CC=C(C=C2)OC)C3=CC=CC=C3
CHEMBL648 acm4_human Human Yes 6.9 Ki = 119 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
266 3 0 2 3.6 CN1CCN(CC1)C(C2=CC=CC=C2)C3=CC=CC=C3
CHEMBL42 acm4_human Human Yes 7.9 Ki = 12.6 Funct
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
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL715 acm4_human Human Yes 7.9 Ki = 12.6 Funct
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
312 1 1 5 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL386983 acm4_human Human No 7.9 Ki = 12.6 Funct
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
532 19 0 14 1.1 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCOCCOC3=NSN=C3OC
CHEMBL42 acm4_human Human Yes 7.9 Ki = 12.6 Funct
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
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL715 acm4_human Human Yes 7.9 Ki = 12.6 Funct
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
312 1 1 5 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL386983 acm4_human Human No 7.9 Ki = 12.6 Funct
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
532 19 0 14 1.1 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCOCCOC3=NSN=C3OC
CHEMBL2114064 acm4_human Human No 7.9 Ki = 12.7 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
437 6 0 5 5.0 COC1=CC=C(C=C1)S(=O)C2=CC=C(C=C2)C(C#N)C3CCN(CC3)C4CCCCC4
CHEMBL215894 acm4_human Human No 6.9 Ki = 120 Funct
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
712 9 3 5 5.9 C1CC(CNC1)CNC(=O)C2CCCN2C(=O)C3CC(CN3C(=O)CC(C4=CC=C(C=C4)Cl)(C5=CC=C(C=C5)Cl)C6=CC=C(C=C6)Cl)O
CHEMBL215894 acm4_human Human No 6.9 Ki = 120 Funct
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
712 9 3 5 5.9 C1CC(CNC1)CNC(=O)C2CCCN2C(=O)C3CC(CN3C(=O)CC(C4=CC=C(C=C4)Cl)(C5=CC=C(C=C5)Cl)C6=CC=C(C=C6)Cl)O
CHEMBL240023 acm4_human Human No 4.9 Ki = 12000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
409 7 0 4 4.4 CCCOC1CCCC2=C1C=C(C=C2)N=CN3CCC4=CC(=C(C=C4C3)OC)OC
CHEMBL391190 acm4_human Human No 4.9 Ki = 12000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
336 3 2 4 3.3 COC1=CC2=C(C=C1)NC3=C2CCNC3CC4=CC5=C(C=C4)OCO5
CHEMBL240023 acm4_human Human No 4.9 Ki = 12000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
409 7 0 4 4.4 CCCOC1CCCC2=C1C=C(C=C2)N=CN3CCC4=CC(=C(C=C4C3)OC)OC
CHEMBL391190 acm4_human Human No 4.9 Ki = 12000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
336 3 2 4 3.3 COC1=CC2=C(C=C1)NC3=C2CCNC3CC4=CC5=C(C=C4)OCO5
CHEMBL21509 acm4_human Human No 4.9 Ki = 12022.6 Funct
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.
276 4 0 2 3.1 CN(C)CCC1=CC(=CC2=CC=CC=N2)C3=CC=CC=C31
CHEMBL21321 acm4_human Human No 5.9 Ki = 1230.3 Funct
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.
358 4 0 4 3.4 C1CN2CCC1C(C2)OC(=O)C3=CC(=CC4=CN=CC=C4)C5=CC=CC=C53
CHEMBL355455 acm4_human Human No 5.9 Ki = 1230.3 Funct
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
318 5 0 2 3.2 CC(C1=CC=CC=N1)C2=C(CC3=CC=CC=C32)CCN4CCCC4
CHEMBL20732 acm4_human Human No 4.9 Ki = 12302.7 Funct
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.
320 6 0 4 2.9 CN(C)CCOC(=O)C1=CC(=CC2=CC=CC=N2)C3=CC=CC=C31
CHEMBL2205827 acm4_human Human No 5.9 Ki = 1233 Funct
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
325 4 1 4 2.3 COC1=C(C=C(C=C1)CN2C3C4C5CC6C4C2(C7C6C5C73)O)OC
CHEMBL2205827 acm4_human Human No 5.9 Ki = 1233 Funct
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
325 4 1 4 2.3 COC1=C(C=C(C=C1)CN2C3C4C5CC6C4C2(C7C6C5C73)O)OC
CHEMBL280684 acm4_human Human No 4.9 Ki = 12589.3 Funct
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.
320 6 0 4 2.8 CN(C)CCOC(=O)C1=CC(=CC2=CN=CC=C2)C3=CC=CC=C31
CHEMBL2432040 acm4_human Human No 5.9 Ki = 1265 Funct
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
279 3 0 2 2.5 CN(CC1=CC=CC=C1)C2C3C4CC5C3C(=O)C6C5C4C62
CHEMBL1734 acm4_human Human Yes 6.9 Ki = 128.8 Funct
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
362 3 0 3 4.0 C1CN2CCC1C(C2)OC(=O)N3CCC4=CC=CC=C4C3C5=CC=CC=C5
CHEMBL171102 acm4_human Human No 6.9 Ki = 128.8 Funct
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
354 6 0 2 3.8 CN(C)CCC1=C(C2=CC=CC=C2C1)C(C3=CC=CC=C3)C4=CC=CC=N4
CHEMBL415 acm4_human Human Yes 7.9 Ki = 13 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
315 4 0 2 5.2 CN(C)CCCN1C2=CC=CC=C2CCC3=C1C=C(C=C3)Cl
CHEMBL445 acm4_human Human Yes 7.9 Ki = 13 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
263 3 1 1 4.5 CNCCC=C1C2=CC=CC=C2CCC3=CC=CC=C31
CHEMBL9967 acm4_human Human Yes 7.9 Ki = 13.8 Funct
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
351 2 1 5 0.1 CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL9967 acm4_human Human Yes 7.9 Ki = 13.8 Funct
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
351 2 1 5 0.1 CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL67532 acm4_rat Rat No 6.9 Ki = 130 Funct
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.
400 4 1 5 0.7 C1CN(CCN1CCCl)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL2205829 acm4_human Human No 5.9 Ki = 1302 Funct
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
309 2 1 4 2.2 C1C2C3C4C1C5C2C6C3C4C5(N6CC7=CC8=C(C=C7)OCO8)O
CHEMBL2205829 acm4_human Human No 5.9 Ki = 1302 Funct
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
309 2 1 4 2.2 C1C2C3C4C1C5C2C6C3C4C5(N6CC7=CC8=C(C=C7)OCO8)O
CHEMBL2432049 acm4_human Human No 5.9 Ki = 1302 Funct
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
266 4 1 2 2.8 C1C2C3CC4C2C5C1C3C(C45)NCCC6=CC=CC=N6
CHEMBL169594 acm4_human Human No 4.9 Ki = 13182.6 Funct
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
322 7 0 4 2.7 CN(C)CCOC(=O)C1=C(C2=CC=CC=C2C1)CC3=CN=CC=C3
CHEMBL104804 acm4_human Human No 5.9 Ki = 1349.0 Funct
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.
411 3 1 3 5.6 CC1=C(C2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)CC6=CC=CC=C6
CHEMBL2112955 acm4_human Human No 7.9 Ki = 14 Funct
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
623 14 3 4 6.3 C1CCC(CC1)CN2CCCC(C2)CNC(=O)CCNC(=O)CNC(=O)CC(C3=CC=CC=C3)(C4=CC=CC=C4)C5=CC=CC=C5
CHEMBL583051 acm4_human Human No 7.9 Ki = 14.1 Funct
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
339 4 1 3 4.4 CN1CCCC1C2=CC=C(O2)C(C3CCCCC3)(C4=CC=CC=C4)O
CHEMBL583051 acm4_human Human No 7.9 Ki = 14.1 Funct
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
339 4 1 3 4.4 CN1CCCC1C2=CC=C(O2)C(C3CCCCC3)(C4=CC=CC=C4)O
CHEMBL105160 acm4_human Human No 7.9 Ki = 14.1 Funct
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.
463 9 1 5 6.3 CCCCCCC1=C(C2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OCC
CHEMBL3354071 acm4_human Human No 7.8 Ki = 14.5 Funct
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
650 20 0 7 9.2 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354071 acm4_human Human No 7.8 Ki = 14.5 Funct
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
650 20 0 7 9.2 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCCCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL2111540 acm4_human Human No 7.8 Ki = 14.8 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
438 6 0 6 4.1 COC1=CC=C(C=C1)S(=O)C2=CC=C(C=C2)C(C#N)N3CCN(CC3)C4CCCCC4
CHEMBL499519 acm4_human Human No 6.9 Ki = 140 Funct
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 receptor expressed in insect Sf9 cells
758 23 5 11 6.2 CCCCCCCCCCCC(C(C)C(=O)NC1CCCCN(C1=O)O)OC(=O)C(CCCCN(C(=O)C)O)NC(=O)C2=COC(=C3C=CC=CC3=O)N2
CHEMBL499519 acm4_human Human No 6.9 Ki = 140 Funct
Binding affinity to human muscarinic M4 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M4 receptor expressed in insect Sf9 cells
758 23 5 11 6.2 CCCCCCCCCCCC(C(C)C(=O)NC1CCCCN(C1=O)O)OC(=O)C(CCCCN(C(=O)C)O)NC(=O)C2=COC(=C3C=CC=CC3=O)N2
CHEMBL241281 acm4_human Human No 5.9 Ki = 1400 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
348 4 0 3 3.6 CC(=O)OC1CCCC2=C1C=C(C=C2)N=CN3CCC4=CC=CC=C4C3
CHEMBL241281 acm4_human Human No 5.9 Ki = 1400 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
348 4 0 3 3.6 CC(=O)OC1CCCC2=C1C=C(C=C2)N=CN3CCC4=CC=CC=C4C3
CHEMBL440138 acm4_human Human No 5.9 Ki = 1400 Funct
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
197 3 0 3 1.8 CCC(=O)OC1CC2CCCC1N2C
CHEMBL12587 acm4_human Human Yes 5.9 Ki = 1400 Funct
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
174 2 1 2 0.1 CC1C(CC(O1)C[N+](C)(C)C)O
CHEMBL12587 acm4_rat Rat Yes 5.9 Ki = 1400 Funct
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
174 2 1 2 0.1 CC1C(CC(O1)C[N+](C)(C)C)O
CHEMBL354841 acm4_human Human No 5.9 Ki = 1412.5 Funct
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
306 5 0 2 3.1 CC1=CC2=C(C=C1)C(=C(C2)CCN(C)C)C(C)C3=CC=CC=N3
CHEMBL1189234 acm4_human Human Yes 5.9 Ki = 1415 Funct
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
265 2 1 2 2.4 C1C2C3C4C1C5C2C6C3C4C5(N6CC7=CC=CC=C7)O
CHEMBL1189234 acm4_human Human Yes 5.9 Ki = 1415 Funct
Inhibition of muscarinic M4 receptor (unknown origin) by PDSP assayInhibition of muscarinic M4 receptor (unknown origin) by PDSP assay
265 2 1 2 2.4 C1C2C3C4C1C5C2C6C3C4C5(N6CC7=CC=CC=C7)O
CHEMBL278129 acm4_human Human No 4.8 Ki = 14791.1 Funct
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.
320 6 0 4 2.8 CN(C)CCOC(=O)C1=CC(=CC2=CC=NC=C2)C3=CC=CC=C31
CHEMBL172234 acm4_human Human No 4.8 Ki = 14791.1 Funct
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
322 7 0 4 2.8 CN(C)CCOC(=O)C1=C(C2=CC=CC=C2C1)CC3=CC=CC=N3
CHEMBL107444 acm4_human Human No 7.8 Ki = 15.1 Funct
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.
406 4 0 5 3.8 CCOC(=O)C1=C(N(C2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=C(C=C5)OC)C)C
CHEMBL420662 acm4_human Human No 7.8 Ki = 15.1 Funct
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.
404 5 1 5 4.2 CC1=C(C2=C(N1)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OCC=C
CHEMBL2115127 acm4_human Human No 7.8 Ki = 15.2 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
426 6 0 5 4.7 COC1=CC=C(C=C1)S(=O)C2=CC=C(C=C2)C(=O)C3CCN(CC3)C4CCCCC4
CHEMBL127273 acm4_human Human No 7.8 Ki = 15.3 Funct
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
687 17 0 6 8.8 COC1=CC=CC=C1CN2CCC(CC2)C3CCN(CC3)CCCCCCCCN4CCC(CC4)C5CCN(CC5)CC6=CC=CC=C6OC
CHEMBL112244 acm4_rat Rat No 7.8 Ki = 15.9 Funct
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
622 24 3 7 4.3 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1C2=CC=CC=C2C(=O)NC3=C1N=CC=C3)CCCCCCN
CHEMBL211976 acm4_human Human No 6.8 Ki = 150 Funct
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
623 10 3 5 4.4 C1CC(N(C1)C(=O)C2CC(CN2C(=O)CC(C3=CC=CC=C3)(C4=CC=CC=C4)C5=CC=CC=C5)O)C(=O)NCCC6CCNCC6
CHEMBL211976 acm4_human Human No 6.8 Ki = 150 Funct
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
623 10 3 5 4.4 C1CC(N(C1)C(=O)C2CC(CN2C(=O)CC(C3=CC=CC=C3)(C4=CC=CC=C4)C5=CC=CC=C5)O)C(=O)NCCC6CCNCC6
CHEMBL524061 acm4_human Human No 5.8 Ki = 1513.6 Funct
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
348 3 0 4 3.5 CN1CCCC1C2CS(=O)C(O2)(C3CCCCC3)C4=CC=CC=C4
CHEMBL3354075 acm4_human Human No 6.8 Ki = 154.9 Funct
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
415 13 1 3 5.7 C1CN(CCC1CCCCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3354075 acm4_human Human No 6.8 Ki = 154.9 Funct
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
415 13 1 3 5.7 C1CN(CCC1CCCCCCCCCO)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL71 acm4_human Human Yes 6.8 Ki = 158.5 Funct
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
319 4 0 3 5.2 CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl
CHEMBL571123 acm4_human Human No 6.8 Ki = 158.5 Funct
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
317 4 0 2 4.8 CN1CCCC1C2=CC=C(O2)C(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL219118 acm4_human Human No 6.8 Ki = 158.5 Funct
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
468 16 0 12 3.2 COC1=NSC(=N1)OCCCOCCCOCCCOC2=NSN=C2C3=CN=CC=C3
CHEMBL376295 acm4_human Human No 6.8 Ki = 158.5 Funct
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
468 16 0 12 2.8 COC1=NSN=C1OCCCOCCCOCCCOC2=NSN=C2C3=CN=CC=C3
CHEMBL71 acm4_human Human Yes 6.8 Ki = 158.5 Funct
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
319 4 0 3 5.2 CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl
CHEMBL571123 acm4_human Human No 6.8 Ki = 158.5 Funct
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
317 4 0 2 4.8 CN1CCCC1C2=CC=C(O2)C(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL407678 acm4_rat Rat No 6.8 Ki = 158.5 Funct
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
1152 27 4 13 5.8 CN(CCCCCCCCN(C)C(=O)CCCCCN(CC(=O)N1C2=CC=CC=C2C(=O)NC3=C1N=CC=C3)CC(=O)N4C5=CC=CC=C5C(=O)NC6=C4N=CC=C6)C(=O)CCCCCNCC(=O)N7C8=CC=CC=C8C(=O)NC9=C7N=CC=C9
CHEMBL219118 acm4_human Human No 6.8 Ki = 158.5 Funct
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
468 16 0 12 3.2 COC1=NSC(=N1)OCCCOCCCOCCCOC2=NSN=C2C3=CN=CC=C3
CHEMBL376295 acm4_human Human No 6.8 Ki = 158.5 Funct
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
468 16 0 12 2.8 COC1=NSN=C1OCCCOCCCOCCCOC2=NSN=C2C3=CN=CC=C3
CHEMBL130835 acm4_human Human No 7.8 Ki = 16.6 Funct
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
715 15 0 6 6.9 COC1=CC=CC=C1CN2CCC(CC2)C3CCN(CC3)C(=O)CCCCCCC(=O)N4CCC(CC4)C5CCN(CC5)CC6=CC=CC=C6OC
CHEMBL241103 acm4_human Human No 5.8 Ki = 1600 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
334 4 0 3 3.2 CC(=O)OC1CCC2=C1C=C(C=C2)N=CN3CCC4=CC=CC=C4C3
CHEMBL241103 acm4_human Human No 5.8 Ki = 1600 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
334 4 0 3 3.2 CC(=O)OC1CCC2=C1C=C(C=C2)N=CN3CCC4=CC=CC=C4C3
CHEMBL978 acm4_rat Rat Yes 5.8 Ki = 1600 Funct
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
160 4 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C
CHEMBL978 acm4_human Human Yes 5.8 Ki = 1600 Funct
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
160 4 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C
CHEMBL104 acm4_human Human Yes 5.8 Ki = 1640 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
345 4 0 1 5.0 C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CN=C4
CHEMBL3770686 acm4_human Human No 5.8 Ki = 1659.6 Funct
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
403 3 2 5 3.6 CC1=C2C(=C(SC2=NC(=C1I)OC)C(=O)NC3CC3)N
CHEMBL1201207 acm4_human Human Yes 5.8 Ki = 1663 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
472 4 4 9 0.1 CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)COP(=O)(O)O)O)C)O)F)C
CHEMBL2112217 acm4_rat Rat No 5.8 Ki = 1670 Funct
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
338 2 2 6 -0.3 C1CN(CCN1)CC(=O)N2C3=C(C=CC=N3)C(=O)NC4=C2N=CC=C4
CHEMBL21716 acm4_human Human No 5.8 Ki = 1698.2 Funct
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.
358 4 0 4 3.5 C1CN2CCC1C(C2)OC(=O)C3=CC(=CC4=CC=CC=N4)C5=CC=CC=C53
CHEMBL169401 acm4_human Human No 5.8 Ki = 1698.2 Funct
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
306 6 0 2 3.1 CC(C1=CC=CC=N1)C2=C(CC3=CC=CC=C32)CCCN(C)C
CHEMBL900 acm4_human Human Yes 7.8 Ki = 17 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
269 6 0 2 3.8 CC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C
CHEMBL253978 acm4_rat Rat Yes 7.8 Ki = 17.4 Funct
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
370 2 1 5 1.7 CC1=C2C(=CS1)C(=O)NC3=CC=CC=C3N2C(=O)CN4CCN(CC4)C
CHEMBL2114067 acm4_human Human No 7.8 Ki = 17.9 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
426 6 0 5 4.7 COC1=CC=C(C=C1)S(=O)C2=CC=C(C=C2)C(=O)C3CCN(CC3)C4CCCCC4
CHEMBL3770686 acm4_human Human No 5.8 Ki = 1700 Funct
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
403 3 2 5 3.6 CC1=C2C(=C(SC2=NC(=C1I)OC)C(=O)NC3CC3)N
CHEMBL3770686 acm4_human Human No 5.8 Ki = 1700 Funct
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
403 3 2 5 3.6 CC1=C2C(=C(SC2=NC(=C1I)OC)C(=O)NC3CC3)N
CHEMBL24369 acm4_human Human No 6.8 Ki = 173 Funct
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
374 12 0 3 6.7 CCN(CC)CCCCCOC(=O)C(C)(C1CCCCC1)C2=CC=CC=C2
CHEMBL301670 acm4_human Human No 6.8 Ki = 173.8 Funct
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
346 2 0 3 5.0 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C
CHEMBL1180343 acm4_human Human No 5.8 Ki = 1730 Funct
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
365 8 0 4 4.0 CCN1CCC(=C(C1)C(=O)OCCC2=CC=C(C=C2)OC)C3=CC=CC=C3
CHEMBL291562 acm4_human Human No 5.8 Ki = 1737.8 Funct
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
344 0 0 3 4.8 CC1CCCC(N1C)C#CC2C3CCCCC3CC4C2C(OC4=O)C
CHEMBL2114066 acm4_human Human No 7.7 Ki = 18.4 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
438 6 0 6 4.1 COC1=CC=C(C=C1)S(=O)C2=CC=C(C=C2)C(C#N)N3CCN(CC3)C4CCCCC4
CHEMBL443780 acm4_human Human Yes 7.7 Ki = 18.5 Funct
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
332 9 0 3 5.6 CCN(CC)CCOC(=O)C(C)(C1CCCCC1)C2=CC=CC=C2
CHEMBL71971 acm4_human Human No 7.7 Ki = 18.6 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
454 6 0 6 4.1 COC1=CC=C(C=C1)S(=O)(=O)C2=CC=C(C=C2)C(C#N)N3CCN(CC3)C4CCCCC4
CHEMBL212141 acm4_human Human No 6.8 Ki = 180 Funct
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
608 8 2 7 4.8 CC(C)NC(=O)C1CCCN1C(=O)C2CC(CN2C(=O)CC(C3=CC=C(C=C3)F)(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)O
CHEMBL212141 acm4_human Human No 6.8 Ki = 180 Funct
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
608 8 2 7 4.8 CC(C)NC(=O)C1CCCN1C(=O)C2CC(CN2C(=O)CC(C3=CC=C(C=C3)F)(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)O
CHEMBL393275 acm4_human Human No 4.8 Ki = 18000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
322 4 2 3 3.4 COC1=CC2=C(C=C1)NC3=C2CCNC3CC4=CC(=CC=C4)OC
CHEMBL393275 acm4_human Human No 4.8 Ki = 18000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
322 4 2 3 3.4 COC1=CC2=C(C=C1)NC3=C2CCNC3CC4=CC(=CC=C4)OC
CHEMBL278074 acm4_human Human No 5.7 Ki = 1819.7 Funct
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.
358 4 0 4 3.4 C1CN2CCC1C(C2)OC(=O)C3=CC(=CC4=CC=NC=C4)C5=CC=CC=C53
CHEMBL2312361 acm4_human Human No 5.7 Ki = 1890 Funct
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
363 6 0 4 3.7 CN1CCC(=C(C1)C(=O)OCCC2=CC3=C(C=C2)OCC3)C4=CC=CC=C4
CHEMBL395110 acm4_human Human Yes 7.7 Ki = 19 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
310 2 0 3 5.6 CN1CCCC(C1)CN2C3=CC=CC=C3SC4=CC=CC=C42
CHEMBL395110 acm4_human Human Yes 7.7 Ki = 19 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
310 2 0 3 5.6 CN1CCCC(C1)CN2C3=CC=CC=C3SC4=CC=CC=C42
CHEMBL136027 acm4_human Human No 7.7 Ki = 20.0 Funct
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
496 17 0 10 6.3 CN1CCC=C(C1)C2=NSN=C2OCCCCCCCCCCCCOC3=NSN=C3OC
CHEMBL335115 acm4_rat Rat No 7.7 Ki = 20.0 Funct
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
650 22 3 7 2.4 CN(CCCCCCCCN(C)C(=O)CCCCCNCC(=O)N1C2=CC=CC=C2C(=O)NC3=C1N=CC=C3)C(=O)CCCCCN
CHEMBL728 acm4_human Human Yes 6.7 Ki = 190 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
374 4 0 4 4.9 CN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL728 acm4_human Human Yes 6.7 Ki = 190 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
374 4 0 4 4.9 CN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL84113 acm4_human Human Yes 6.7 Ki = 190 Funct
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
231 3 1 3 2.5 C1CC2CC(C(C1)N2)OC(=O)C3=CC=CC=C3
CHEMBL105945 acm4_human Human No 6.7 Ki = 190.6 Funct
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.
392 3 0 5 3.5 CC1=C(C2=C(N1C)C=CC3=C2CN4CCC5=C(C4O3)C=CC(=C5)OC)C(=O)OC
CHEMBL392888 acm4_human Human No 4.7 Ki = 19000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
280 4 1 2 2.6 CN(CC1=CC=CC=C1)C=NC2=CC3=C(CCC3O)C=C2
CHEMBL392888 acm4_human Human No 4.7 Ki = 19000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
280 4 1 2 2.6 CN(CC1=CC=CC=C1)C=NC2=CC3=C(CCC3O)C=C2
CHEMBL355392 acm4_human Human No 5.7 Ki = 1905.5 Funct
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
332 5 0 2 3.5 CC(C1=CC=CC=N1)C2=C(CC3=CC=CC=C32)CCN4CCCCC4
CHEMBL1306 acm4_human Human Yes 5.7 Ki = 1913 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
532 8 0 7 4.8 CC(C)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=NC=N4)C5=C(C=C(C=C5)Cl)Cl
CHEMBL1306 acm4_human Human Yes 5.7 Ki = 1913 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
532 8 0 7 4.8 CC(C)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=NC=N4)C5=C(C=C(C=C5)Cl)Cl
CHEMBL3770870 acm4_human Human No 6.7 Ki = 195.0 Funct
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
326 4 2 5 3.9 CCOC1=C(C(=C2C(=C(SC2=N1)C(=O)NC3CC3)N)C)Cl
CHEMBL3770870 acm4_human Human No 6.7 Ki = 195.0 Funct
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
326 4 2 5 3.9 CCOC1=C(C(=C2C(=C(SC2=N1)C(=O)NC3CC3)N)C)Cl
CHEMBL430587 acm4_human Human No 5.7 Ki = 1949.8 Funct
Binding affinity against human muscarine receptor (hM4) cloned in CHO cellsBinding affinity against human muscarine receptor (hM4) cloned in CHO cells
344 0 0 3 4.8 CC1CCCC(N1C)C#CC2C3CCCCC3CC4C2C(OC4=O)C
CHEMBL105593 acm4_human Human No 5.7 Ki = 1949.8 Funct
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.
397 3 1 4 4.5 CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=CC=C5Cl)C
CHEMBL352723 acm4_human Human No 5.7 Ki = 1995.3 Funct
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
339 6 0 3 3.2 CC(C1=CC=CC=N1)C2=C(CC3=C2C=C(C=C3)SC)CCN(C)C
CHEMBL307810 acm4_human Human No 8.7 Ki = 2.2 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
427 6 0 5 4.5 CC(C1=CC=C(C=C1)S(=O)C2=CC=C(C=C2)OC)N3CCN(CC3)C4CCCCC4
CHEMBL2112957 acm4_human Human No 8.6 Ki = 2.3 Funct
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
689 11 1 4 7.8 C1CCC(CC1)CN2CCCC(C2)CNC(=O)C3CCCN3C(=O)C4CCCN4C(=O)CC(C5=CC=CC=C5)(C6=CC=CC=C6)C7=CC=CC=C7
CHEMBL385328 acm4_human Human No 8.6 Ki = 2.3 Funct
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
332 3 0 3 5.0 CN1CCCC1C2CSC(O2)(C3CCCCC3)C4=CC=CC=C4
CHEMBL385328 acm4_human Human No 8.6 Ki = 2.3 Funct
Binding affinity to human cloned muscarinic receptor M4 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M4 expressed in CHO cells
332 3 0 3 5.0 CN1CCCC1C2CSC(O2)(C3CCCCC3)C4=CC=CC=C4
CHEMBL216927 acm4_human Human Yes 8.6 Ki = 2.5 Funct
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
488 16 0 13 1.2 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCOC3=NSN=C3OC
CHEMBL216927 acm4_human Human Yes 8.6 Ki = 2.5 Funct
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
488 16 0 13 1.2 CN1CCC=C(C1)C2=NSN=C2OCCOCCOCCOCCOC3=NSN=C3OC
CHEMBL1626 acm4_human Human Yes 8.6 Ki = 2.8 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
344 6 0 2 5.0 CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCC3CCCN3C
CHEMBL378772 acm4_human Human No 7.7 Ki = 20 Funct
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
717 11 2 8 5.5 C1CC(N(C1)C(=O)C2CC(CN2C(=O)CC(C3=CC=C(C=C3)F)(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)O)C(=O)NCC6CCN(CC6)CC7CC7
CHEMBL378772 acm4_human Human No 7.7 Ki = 20 Funct
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
717 11 2 8 5.5 C1CC(N(C1)C(=O)C2CC(CN2C(=O)CC(C3=CC=C(C=C3)F)(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)O)C(=O)NCC6CCN(CC6)CC7CC7
CHEMBL240022 acm4_human Human No 6.7 Ki = 200 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
408 6 0 5 3.5 CC(=O)OC1CCCC2=C1C=C(C=C2)N=CN3CCC4=CC(=C(C=C4C3)OC)OC
CHEMBL241102 acm4_human Human No 6.7 Ki = 200 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
394 6 0 5 3.2 CC(=O)OC1CCC2=C1C=C(C=C2)N=CN3CCC4=CC(=C(C=C4C3)OC)OC
CHEMBL392970 acm4_human Human No 6.7 Ki = 200 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
423 6 0 5 4.1 CC(=O)OC1CCCCC2=C1C=C(C=C2)N=CN3CCC4=CC(=C(C=C4C3)OC)OC
CHEMBL3770870 acm4_human Human No 6.7 Ki = 200 Funct
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
326 4 2 5 3.9 CCOC1=C(C(=C2C(=C(SC2=N1)C(=O)NC3CC3)N)C)Cl
CHEMBL240022 acm4_human Human No 6.7 Ki = 200 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
408 6 0 5 3.5 CC(=O)OC1CCCC2=C1C=C(C=C2)N=CN3CCC4=CC(=C(C=C4C3)OC)OC
CHEMBL241102 acm4_human Human No 6.7 Ki = 200 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
394 6 0 5 3.2 CC(=O)OC1CCC2=C1C=C(C=C2)N=CN3CCC4=CC(=C(C=C4C3)OC)OC
CHEMBL392970 acm4_human Human No 6.7 Ki = 200 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
423 6 0 5 4.1 CC(=O)OC1CCCCC2=C1C=C(C=C2)N=CN3CCC4=CC(=C(C=C4C3)OC)OC
CHEMBL241101 acm4_human Human No 5.7 Ki = 2000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
395 5 0 5 2.8 COC1=C(C=C2CN(CCC2=C1)C=NC3=CC4=C(CCN4C(=O)OC)C=C3)OC
CHEMBL441356 acm4_human Human Yes 5.7 Ki = 2000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
354 2 0 4 3.1 C[N+]12CCC3=CC4=C(C=C3C1CC5=C(C2)C(=C(C=C5)OC)OC)OCO4
CHEMBL241101 acm4_human Human No 5.7 Ki = 2000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
395 5 0 5 2.8 COC1=C(C=C2CN(CCC2=C1)C=NC3=CC4=C(CCN4C(=O)OC)C=C3)OC
CHEMBL441356 acm4_human Human Yes 5.7 Ki = 2000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
354 2 0 4 3.1 C[N+]12CCC3=CC4=C(C=C3C1CC5=C(C2)C(=C(C=C5)OC)OC)OCO4
CHEMBL285898 acm4_human Human No 6.7 Ki = 209 Funct
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
360 11 0 3 6.3 CCN(CC)CCCCOC(=O)C(C)(C1CCCCC1)C2=CC=CC=C2
CHEMBL71 acm4_human Human Yes 7.7 Ki = 21 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
319 4 0 3 5.2 CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl
CHEMBL519609 acm4_human Human No 7.7 Ki = 21 Funct
Antagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M4 receptor (unknown origin) by PDSP assay
356 7 0 4 4.5 CCN(CC)CCCOC(=O)N1C2=CC=CC=C2SC3=CC=CC=C31
CHEMBL71 acm4_human Human Yes 7.7 Ki = 21 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
319 4 0 3 5.2 CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl
CHEMBL304112 acm4_rat Rat No 6.7 Ki = 210 Funct
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
539 7 1 7 1.5 C1CN(CCN1CCCCN2C(=O)C3=CC=CC=C3C2=O)CC(=O)N4C5=CC=CC=C5C(=O)NC6=C4N=CC=C6
CHEMBL279520 acm4_human Human No 4.7 Ki = 21379.6 Funct
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.
319 5 1 3 2.3 CN(C)CCNC(=O)C1=CC(=CC2=CN=CC=C2)C3=CC=CC=C31
CHEMBL481 acm4_human Human Yes 6.7 Ki = 217 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
587 5 1 8 3.0 CCC1=C2C=C(C=CC2=NC3=C1CN4C3=CC5=C(C4=O)COC(=O)C5(CC)O)OC(=O)N6CCC(CC6)N7CCCCC7
CHEMBL481 acm4_human Human Yes 6.7 Ki = 217 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
587 5 1 8 3.0 CCC1=C2C=C(C=CC2=NC3=C1CN4C3=CC5=C(C4=O)COC(=O)C5(CC)O)OC(=O)N6CCC(CC6)N7CCCCC7
CHEMBL715 acm4_human Human Yes 7.7 Ki = 22 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
312 1 1 5 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL55 acm4_human Human Yes 6.7 Ki = 220 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
340 10 4 4 2.6 C1=CC(=CC=C1C(=N)N)OCCCCCOC2=CC=C(C=C2)C(=N)N
CHEMBL55 acm4_human Human Yes 6.7 Ki = 220 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
340 10 4 4 2.6 C1=CC(=CC=C1C(=N)N)OCCCCCOC2=CC=C(C=C2)C(=N)N
CHEMBL67381 acm4_rat Rat No 6.7 Ki = 220 Funct
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
428 4 1 5 1.6 C1CN(CCN1CC2=CC=CC=C2)CC(=O)N3C4=CC=CC=C4C(=O)NC5=C3N=CC=C5
CHEMBL82754 acm4_human Human No 5.7 Ki = 2200 Funct
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
237 3 1 3 2.9 C1CCC(CC1)C(=O)OC2CC3CCCC2N3
CHEMBL275104 acm4_human Human No 6.7 Ki = 222 Funct
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
208 2 0 3 0.1 C1CCN(C1)CC#CCN2C(=O)CCO2
CHEMBL275104 acm4_human Human No 6.7 Ki = 222 Funct
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
208 2 0 3 0.1 C1CCN(C1)CC#CCN2C(=O)CCO2
CHEMBL21508 acm4_human Human No 4.7 Ki = 22387.2 Funct
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.
276 4 0 2 3.1 CN(C)CCC1=CC(=CC2=CN=CC=C2)C3=CC=CC=C31
CHEMBL7002 acm4_human Human Yes 5.6 Ki = 2263 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
333 5 1 4 4.8 CC1(CCCCC1)COC2=CC=C(C=C2)CC3C(=O)NC(=O)S3
CHEMBL12587 acm4_human Human Yes 7.6 Ki = 23 Funct
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
174 2 1 2 0.1 CC1C(CC(O1)C[N+](C)(C)C)O
CHEMBL303684 acm4_rat Rat No 7.6 Ki = 23.2 Funct
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
537 11 2 7 2.2 CC(C)(C)OC(=O)NCCCCCCN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL954 acm4_human Human Yes 6.6 Ki = 230 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
406 9 0 2 7.2 CCN(CC)CCOC1=CC=C(C=C1)C(=C(C2=CC=CC=C2)Cl)C3=CC=CC=C3
CHEMBL314493 acm4_human Human No 5.6 Ki = 2300 Funct
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
317 4 0 4 3.6 CN1C2CCCC1C(C2)OC(=O)OCC(Cl)(Cl)Cl
CHEMBL2205813 acm4_human Human No 5.6 Ki = 2338 Funct
Binding affinity to M4 muscarinic receptorBinding affinity to M4 muscarinic receptor
339 5 1 4 2.8 COC1=CC=CC(=C1OC)CCN2C3C4C5CC6C4C2(C7C6C5C73)O
CHEMBL169494 acm4_human Human No 5.6 Ki = 2398.8 Funct
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
278 5 0 2 2.4 CN(C)CCC1=C(C2=CC=CC=C2C1)CC3=CC=CC=N3
CHEMBL378859 acm4_human Human No 7.6 Ki = 24 Funct
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
726 10 3 5 6.2 C1CC(N(C1)C(=O)C2CC(CN2C(=O)CC(C3=CC=C(C=C3)Cl)(C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl)O)C(=O)NCCC6CCNCC6
CHEMBL378859 acm4_human Human No 7.6 Ki = 24 Funct
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
726 10 3 5 6.2 C1CC(N(C1)C(=O)C2CC(CN2C(=O)CC(C3=CC=C(C=C3)Cl)(C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl)O)C(=O)NCCC6CCNCC6
CHEMBL7303 acm4_human Human Yes 5.6 Ki = 2400 Funct
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
155 2 0 3 0.3 CN1CCC=C(C1)C(=O)OC
CHEMBL7303 acm4_rat Rat Yes 5.6 Ki = 2400 Funct
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
155 2 0 3 0.3 CN1CCC=C(C1)C(=O)OC
CHEMBL7303 acm4_human Human Yes 5.6 Ki = 2400 Funct
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
155 2 0 3 0.3 CN1CCC=C(C1)C(=O)OC
CHEMBL328476 acm4_human Human No 4.6 Ki = 24000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
306 2 2 3 3.3 C1CNC(C2=C1C3=CC=CC=C3N2)CC4=CC5=C(C=C4)OCO5
CHEMBL328476 acm4_human Human No 4.6 Ki = 24000 Funct
Displacement of [3H]N-methylscopolamine from muscarinic M4 receptorDisplacement of [3H]N-methylscopolamine from muscarinic M4 receptor
306 2 2 3 3.3 C1CNC(C2=C1C3=CC=CC=C3N2)CC4=CC5=C(C=C4)OCO5
CHEMBL1113 acm4_human Human Yes 6.6 Ki = 242 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
314 1 1 3 2.6 C1CN(CCN1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl
CHEMBL478227 acm4_human Human No 5.6 Ki = 2454.7 Funct
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
406 2 1 5 1.4 CN1CCN(C2C1CCCC2)CC(=O)N3C4=CC=CC=C4C(=O)NC5=C3N=CC=C5
CHEMBL478227 acm4_human Human No 5.6 Ki = 2454.7 Funct
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
406 2 1 5 1.4 CN1CCN(C2C1CCCC2)CC(=O)N3C4=CC=CC=C4C(=O)NC5=C3N=CC=C5
CHEMBL513277 acm4_human Human No 4.6 Ki = 24547.1 Funct
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
165 1 0 2 1.8 CC1=CC=C(O1)C2CCCN2C
CHEMBL283320 acm4_human Human No 4.6 Ki = 24547.1 Funct
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.
319 5 1 3 2.3 CN(C)CCNC(=O)C1=CC(=CC2=CC=NC=C2)C3=CC=CC=C31
CHEMBL513277 acm4_human Human No 4.6 Ki = 24547.1 Funct
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
165 1 0 2 1.8 CC1=CC=C(O1)C2CCCN2C
CHEMBL216928 acm4_human Human No 7.6 Ki = 25.1 Funct
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
488 16 0 13 2.1 CN1CCC=CC1C2=NSN=C2OCCOCCOCCOCCOC3=NC(=NS3)OC
CHEMBL216928 acm4_human Human No 7.6 Ki = 25.1 Funct
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
488 16 0 13 2.1 CN1CCC=CC1C2=NSN=C2OCCOCCOCCOCCOC3=NC(=NS3)OC
CHEMBL608151 acm4_human Human No 6.6 Ki = 251.2 Funct
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
286 4 1 2 3.1 CCOCC1C2C1(CNC2)C3=CC(=C(C=C3)Cl)Cl
CHEMBL608151 acm4_human Human No 6.6 Ki = 251.2 Funct
Inhibition of muscarinic M4 receptorInhibition of muscarinic M4 receptor
286 4 1 2 3.1 CCOCC1C2C1(CNC2)C3=CC(=C(C=C3)Cl)Cl
CHEMBL294649 acm4_human Human No 4.6 Ki = 25118.9 Funct
Binding affinity against Muscarinic acetylcholine receptor M4Binding affinity against Muscarinic acetylcholine receptor M4
311 3 1 3 1.8 CN1C=C(C2=CC=CC=C21)C(=O)C(=O)NC3CN4CCC3CC4
CHEMBL496915 acm4_human Human No 6.6 Ki = 257.0 Funct
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
348 3 0 4 3.5 CN1CCCC1C2CS(=O)C(O2)(C3CCCCC3)C4=CC=CC=C4
CHEMBL70003 acm4_rat Rat No 5.6 Ki = 2570 Funct
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
422 5 2 6 -0.6 CC(=O)NCCN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
CHEMBL1258452 acm4_human Human No 5.6 Ki = 2579 Funct
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
320 8 1 5 3.1 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C=C2)N)OC
CHEMBL1258452 acm4_human Human No 5.6 Ki = 2579 Funct
Binding affinity to human muscarinic M4 receptorBinding affinity to human muscarinic M4 receptor
320 8 1 5 3.1 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C=C2)N)OC
CHEMBL296419 acm4_human Human Yes 6.6 Ki = 259 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
459 8 1 5 6.0 COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
CHEMBL7303 acm4_human Human Yes 7.6 Ki = 26 Funct
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
155 2 0 3 0.3 CN1CCC=C(C1)C(=O)OC
CHEMBL3354066 acm4_human Human No 7.6 Ki = 26.3 Funct
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
510 10 0 7 3.8 CN1CCC=C(C1)C2=NSN=C2OCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3354066 acm4_human Human No 7.6 Ki = 26.3 Funct
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
510 10 0 7 3.8 CN1CCC=C(C1)C2=NSN=C2OCCCC3CCN(CC3)CCCN4C(=O)CCC5=CC=CC=C54
CHEMBL3769740 acm4_human Human No 5.6 Ki = 2691.5 Funct
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
354 6 2 5 4.8 CCCCOC1=C(C(=C2C(=C(SC2=N1)C(=O)NC3CC3)N)C)Cl
CHEMBL3769740 acm4_human Human No 5.6 Ki = 2691.5 Funct
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
354 6 2 5 4.8 CCCCOC1=C(C(=C2C(=C(SC2=N1)C(=O)NC3CC3)N)C)Cl
CHEMBL352779 acm4_human Human No 4.6 Ki = 26915.4 Funct
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
321 6 1 3 2.2 CN(C)CCNC(=O)C1=C(C2=CC=CC=C2C1)CC3=CC=CC=N3
CHEMBL3769740 acm4_human Human No 5.6 Ki = 2700 Funct
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
354 6 2 5 4.8 CCCCOC1=C(C(=C2C(=C(SC2=N1)C(=O)NC3CC3)N)C)Cl
CHEMBL7568 acm4_human Human Yes 6.6 Ki = 277 Funct
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
400 9 1 4